BRPI0714469A2 - nf-kappab inhibitors - Google Patents

Abstract

NF-KAPPA-B Inhibitors. The present invention provides an NF-KB inhibitor. The NF-KB inhibitor of the present invention contains a carbostyril compound represented by General Formula (1) or a salt thereof, wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group; X is an oxygen atom or a sulfur atom; R 4 and R 5 each of which represent a hydrogen atom; the bond between positions 3 and 4 of the carbostyril backbone is a single bond or a double bond; R4 is a hydrogen atom, etc .; R2 is a hydrogen atom, etc .; and R3 is a hydrogen atom, etc.

Description

Patent Descriptive Report for "NF-kappaB Inhibitors". TECHNICAL FIELD

The present invention relates to an NF-κB inhibitor.

BACKGROUND TECHNIQUE

NF-κΒ, a substance known to be one of such transcriptional regulatory factors, is a heterodimer of p65 and p50 proteins. In cytoplasm, NF-κΒ is generally present as a substance that binds with IkB, an inhibiting factor, and thus prevents nucleus migration. However, when the cell is stimulated by cytokines, ischemia, or reperfusion for any reason, IkB is phosphorylated and decomposed so that NF-κΒ is activated and penetrated into the nucleus. NF-κΒ binds by itself to the chromosome NF-κΒ binding site and then promotes transcription of the downstream localized gene. The NF-κΒ controlled gene includes cytokines such as TNF-α, IL-2, IL-1, IL-6, IL-8, etc. and adhesion factors such as VCAM-1, ICAM-1, etc.

Two isomers, COX-1 and COX-2, are known as the cyclooxygenase (COX) enzyme. COX-1 is primarily known to be involved in gastrointestinal membrane protection, etc., while COX-2 is known to be involved in inflammation and pain. Therefore, pharmaceutical agents having COX-2 inhibitory activity are known to exhibit anti-inflammatory, anti-pyrogenic, and analgesic effects.

It is also known that compounds having COX-2 inhibitory activity exhibit radiosensitivity enhancing effect on radiotherapy (Cancer Research 60, 1326-1331, March 1, 2000; Clinical Cancer Research, Vol. 7, 2998-3005, October 2001; etc.), and tumor-induced angiogenesis inhibitor (BMC Cancer, January 12, 2006 6: 9; Breast Cancer Reseach, Vol.7 No.4, R422-35; etc.).

A carbostyril compound capable of inducing TFF production is also known (W02006 / 035954). It is also known that carbostyril compound which has the action of inducing TFF production is useful in preventing or treating eye diseases (such as dry eye, corneal ulcer, corneal infiltration, corneal perforation, keratitis, punctate keratopathy). corneal epithelial defects, corneal erosion, recurrent corneal erosion, persistent corneal epithelial defects, corneal opacity, conjunctivitis, conjunctival epithelial defects, dry keratoconjunctivitis, and upper filament keratitis).

However, it is not known whether such a carboxytyl compound has NF-κΒ inhibitory activity and / or COX-2 inhibitory activity. DESCRIPTION OF THE INVENTION

An object of the present invention is to provide a preventive or therapeutic agent for NF-κB associated disease.

The present inventors have performed extensive research on carbostyril compounds represented by the General Formula (1) shown below, and found that carbostyril compounds exhibit NF-κΒ inhibitory activity, and / or COX-2 inhibitory activity, especially inhibitory activity. COX-2 production line. The present invention has been accompanied on the basis of this discovery.

The present invention provides pharmaceutical compositions, methods, and use described in items 1 to 34 below:

1. A preventive or therapeutic agent for an NF-κΒ-associated disease comprising as an active ingredient a carbostyril compound represented by General Formula (1)

or a salt of this,

wherein A is a direct bond, a lower alkylene group, or a lower alkylidene group;

the bond between positions 3 and 4 of the carbostyril backbone is a single bond or a double bond;

R4 and R5 each represents a hydrogen atom with the

(1)

25

X is an oxygen atom or a sulfur atom; provided that when the bond between positions 3 and 4 of the carbostyril backbone is a double bond, R 4 and R 5 may instead be joined together as a group -CH = CH-CH = CH-;

R1 is one of the following (1 -1) to (1-30): (1-1) a hydrogen atom,

(1-2) a lower alkyl group,

(1-3) a lower phenyl alkyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of a phenyl group, lower alkyl groups, lower alkoxy groups, halogen atoms, groups - (B) ^ NR6R7 , a nitro group, a carboxy group, lower alkoxycarbonyl groups, a cyano group, lower alkoxyphenyl groups, a phaenoxy group, lower alkoxycarbonyl piperidinyl groups, lower amino alkoxycarbonyl groups optionally substituted by one or more cycloalkyl groups; 2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring with one or more lower alkylthio groups, 3-pyrrolinylcarbonyl groups optionally substituted on the 3-pyrroline ring with one or more lower alkyl groups, thiazolidinylcarbonyl groups optionally substituted on the thiazole ring; dine with a phenyl group, 3-azabicyclo [3,2,2] nonylcarbonyl groups, lower alkyl piperidinyl groups, lower alkyl anilino groups amino group having one or more lower alkyl groups, lower alkylphenyl groups, indolinyl lower alkyl groups, and optionally substituted piperidinylcarbonyl groups on the piperidine ring with one or more lower alkyl groups,

(1-4) a lower cycloalkyl alkyl group, (1-5) a lower alkyl phenoxy group,

(1-6) a lower alkyl naphthyl group, (1-7) a lower alkyl lower alkoxy group, (1-8) a lower alkyl carboxy group, (1-9) a lower alkyl alkoxycarbonyl group, (1-10) an optionally substituted lower alkyl pyridyl group

the pyridine ring with one or more members selected from the group consisting of halogen atoms; piperidinyl groups; a morpholino group; piperazinyl groups optionally substituted on the piperazine ring with one or more members selected from the group consisting of a phenyl group and lower alkyl group; thienyl groups; a phenyl group; pyridyl groups; piperidinyl lower alkyl groups; phenyl lower alkyl groups; biphenyl groups; lower alkyl groups optionally substituted with one or more halogen atoms; pyridylamino groups; pyridylcarbonylamino groups; lower alkoxy groups; lower alkyl anilino groups optionally substituted on the amino group with one or more lower alkyl groups; and anilino groups optionally substituted on the amino group with one or more lower alkyl groups, (1-11) a lower alkyl cyano group,

lower cab,

(1-17) a hydroxy-substituted lower alkyl group, (1-18) a thiazolyl lower alkyl group optionally substituted on the triazole ring with one or more members selected from the group consisting of halogen atoms, a phenyl group, thienyl groups, and pyridyl groups,

(1-19) a lower alkyl group optionally substituted with one or more halogen atoms,

(1-20) a lower alkyl alkylsilyloxy group, (1-21) a lower alkyl phenoxy group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms ; lower alkoxy groups; halogen atoms; lower alkenyl groups; cycloalkyl groups; a nitro group; and a phenyl group,

(1-22) a lower alkyl phenylthio group optionally substituted on the phenyl ring having one or more halogen atoms,

(1-12) a group -Ai-CONR8R9, (1-13) a group of the following Formula

15

(1-14) a phenyl group,

(1-15) a lower alkyl quinolyl group,

(1-16) a lower alkyl group substituted by lower alkoxy al- (1-23) lower alkylpiperidinyl groups optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl phenyl groups and a phenyl group,

(1-24) a lower alkyl piperazinyl group optionally substituted on the piperazine ring with one or more phenyl groups,

(1-25) a lower alkyl 1,2,3,4-tetrahydroisoquinolyl group, (1-26) a lower alkyl naphthyloxy group,

(1-27) a lower alkyl benzothiazolyloxy group optionally substituted on the benzothiazole ring with one or more alkyl groups, (1-28) a lower alkyl group substituted with one or more

selected members of the group consisting of quinolyloxy groups and isoquinolyloxy groups,

(1-29) a lower alkyl pyridyloxy group optionally substituted on the pyridine ring with one or more lower alkyl groups, (1-30) a lower alkenyl;

R 2 is one of the following (2-1) to (2-33): (2-1) a hydrogen atom, (2-2) a lower alkoxy group, (2-3) a lower alkyl group, (2- 4) a lower alkoxy carboxy group,

(2-5) a lower alkoxy group lower alkoxycarbonyl, (2-6) a hydroxy group,

(2-7) a phenyl lower alkoxy group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; lower alkylthio groups optionally substituted with one or more halogen atoms; lower alkoxy groups; a nitro group; lower alkylsulfonyl groups; lower alkoxycarbonyl groups; phenyl lower alkenyl groups; lower alkanoyloxy groups; and 1,2,3-thiadiazolyl groups,

(2-8) a lower alkoxy piperidinyl group optionally substituted on the piperidine ring with one or more lower alkyl groups, (2-9) an amino-substituted lower alkoxy group optionally substituted with one or more lower alkyl groups, ( 2-10) a lower alkenyloxy group,

(2-11) a pyridyl lower alkoxy group optionally substituted on the pyridine ring with one or more lower alkyl groups, each substituted with lower alkyl optionally substituted with one or more halogen atoms,

(2-12) a lower alkynyloxy group, (2-13) a phenyl lower alkynyloxy group, (2-14) a phenyl lower alkenyloxy group,

(2-15) a lower alkoxy furyl group optionally substituted on the furan ring with one or more lower alkoxycarbonyl groups,

(2-16) a tetrazolyl lower alkoxy group optionally substituted on the tetrazol ring with a member selected from the group consisting of a phenyl group, lower phenyl alkyl groups, and lower cycloalkyl alkyl groups,

(2-17) a 1,2,4-oxadiazolyl lower alkoxy group optionally substituted on the 1,2,4-oxadiazole ring with a phenyl group, the phenyl substituent optionally being substituted on the phenyl ring with one or more alkyl groups bottom,

(2-18) an isoxazolyl lower alkoxy group optionally substituted on the isoxazole ring with one or more lower alkyl groups,

(2-19) a lower alkoxy group 1,3,4-oxadiazolyl optionally substituted on the 1,3,4-oxadiazole ring with a phenyl group, the phenyl substituent optionally being substituted on the phenyl ring with one or more alkyl groups bottom,

(2-20) a lower alkoxy group lower alkanoyl, (2-21) a thiazolyl lower alkoxy group optionally substituted on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and one phenyl group, each phenyl opio substituent - optionally being substituted on the phenyl ring with one or more halogen atoms, (2-22) a piperidinoxy group optionally substituted on the piperidine ring with one or more benzoyl groups, each benzoyl substituent optionally being substituted on the phenyl ring with one or more atoms halogen,

(2-23) a thienyl lower alkoxy group,

(2-24) a lower alkoxy phenylthio group,

(2-25) a lower alkoxy group substituted by carbamoyl optionally substituted with one or more lower alkyl groups, (2-26) a lower benzoyl alkoxy group, (2-27) a lower alkoxy pyridylcarbonyl group,

(2-28) an imidazolyl lower alkoxy group optionally substituted on the imidazole ring with one or more phenyl lower alkyl groups, (2-29) a lower alkoxy phenoxy group,

(2-30) a lower alkoxy group substituted by phenyl lower alkoxy, (2-31) a 2,3-dihydro-1H-indenyloxy group,

(2-32) an isoindolinyl lower alkoxy group optionally substituted on the isoindoline ring with one or more oxo groups, (2-33) a phenyl group; R3 is one of the following (3-1) to (3-19): (3-1) a hydrogen atom,

(3-2) a lower alkyl group, (3-3) a hydroxy-substituted lower alkyl group, (3-4) a lower cycloalkyl alkyl group, (3-5) a lower alkyl carboxy group, (3-6) a lower alkyl alkoxycarbonyl group,

(3-7) a phenyl lower alkyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups optionally substituted with one or more halogen atoms; a phenyl group; lower alkoxycarbonyl groups; a phenoxy group; lower alkylthio groups; lower alkylsulfonyl groups; phenyl lower alkoxy groups; and nitro groups optionally substituted with one or more lower alkanoyl groups, (3-8) a lower alkyl naphthyl group,

(3-9) an optionally substituted lower alkyl furyl group on the furan ring with one or more lower alkoxycarbonyl groups, (3-10) an optionally substituted thiazolyl lower alkyl group

on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and one phenyl group, each phenyl substituent optionally being substituted on the phenyl ring with one or more optionally halogen substituted lower alkyl groups, (3-11) an optionally substituted lower alkyl tetrazolyl group

tetrazole ring with one or more lower alkyl groups,

(3-12) a benzothienyl lower alkyl group optionally substituted on the benzothiophene ring with one or more halogen atoms, (3-13) a lower alkynyl group, (3-14) a lower alkenyl group,

(3-15) a lower alkenyl phenyl group, (3-16) a lower alkyl benzoimidazolyl group, (3-17) a lower alkyl pyridyl group,

(3-18) a lower alkyl imidazole group optionally substituted on the imidazole ring with one or more phenyl lower alkyl groups; (3-19) a quinolyl lower alkyl group; B is a carbonyl group or an -NHCO- group; I is 0 or 1;

R 6 and R 7 each independently represent one of the following (4-1) to (4-79):

(4-1) a hydrogen atom, (4-2) a lower alkyl group, (4-3) a lower alkanoyl group,

(4-4) a lower alkylsulfonyl group optionally substituted by one or more halogen atoms,

(4-5) an alkoxycarbonyl group optionally substituted with one or more halogen atoms, (4-6) a hydroxy substituted lower alkyl group, (4-7) an pyridylcarbonyl group optionally substituted on the pyridine ring with one or more selected members of the group consisting of pyrrolyl groups and halogen atoms, (4-8) a pyridyl group optionally substituted on the pyridine ring

with one or more members selected from the group consisting of lower alkyl groups and lower alkoxy groups,

(4-9) a lower alkyl pyridyl group,

(4-10) a phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; a phenoxy group; lower alkoxy groups optionally substituted with one or more halogen atoms; lower alkylthio groups; lower alkylsulfonyl groups; amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups; pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups; piperidinyl groups optionally substituted on the piperidine ring with one or more lower alkyl groups; lower alkenyl groups; an aminosulfonyl group; a hydroxy group; carbamoyl groups optionally substituted by one or more lower alkyl groups; phenyl lower alkoxy groups; and a cyan group,

(4-11) a cycloalkyl group optionally substituted on the cycloalkyl ring with one or more lower alkyl groups,

(4-12) a benzoyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; a phenoxy group; a phenyl group; lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups; lower alkanoyl groups; a nitro group; a cyan group; amino groups optionally substituted with one or more members selected from the group consisting of a phenyl group and lower alkyl groups; pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups; pyrrolyl groups; pyrazolyl groups; 1,2,4-triazolyl groups; and imidazolyl groups,

(4-13) a phenyl ring substituted benzoyl group with one or more lower alkylenedioxy groups,

(4-14) a cycloalkylcarbonyl group, (4-15) a furylcarbonyl group,

(4-16) a naphthylcarbonyl group,

(4-17) a phenoxycarbonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxy groups, lower alkyl groups, halogen atoms, and a nitro group,

(4-18) a lower phenyl alkoxycarbonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and a nitro group,

(4-19) a piperidinyl group optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl group; lower alkanoyl groups; optionally substituted benzoyl groups on the phenyl ring having one or more halogen atoms; and optionally substituted phenyl groups on the phenyl ring having one or more halogen atoms,

(4-20) a lower alkyl tetrahydropyranyl group,

(4-21) a lower cycloalkyl alkyl group, (4-22) a lower alkenyl group,

(4-23) a lower alkyl phenyl group optionally substituted on the alkyl group with one or more lower alkoxycarbonyl groups; and optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms, lower alkyl groups optionally substituted with one or more halogen atoms, lower alkoxy groups optionally substituted with one or more halogen atoms halogen, and a hydroxy group,

(4-24) a lower alkylene phenyl group substituted by alkylenedioxy.

bottom xi,

(4-25) a lower alkyl furyl group, (4-26) a lower alkyl carbamoyl group optionally substituted with one or more members selected from lower alkyl groups and a phenyl group, each phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups, (4-27) a lower alkyl lower alkoxy group,

(4-28) a lower alkyl imidazole group optionally substituted on the lower alkyl group with one or more members selected from the group consisting of a carbamoyl group and lower alkoxycarbonyl groups,

(4-29) an amino-substituted lower alkyl group optionally substituted with one or more lower alkyl groups,

(4-30) a 2,3,4,5-tetrahydrofuran group optionally substituted on the 2,3,4,5-tetrahydrofuran ring with one or more oxo groups, (4-31) a lower alkyl alkoxycarbonyl group, (4- 32) a lower alkyl pyrrolidinyl group optionally substituted on the pyrrolidine ring with one or more lower alkyl groups, (4-33) a lower alkanoyl phenoxy group, (4-34) a lower alkyl morpholino group, (4-35) a indolyl group, (4-36) a thiazolyl group, (4-37) a 1,2,4-triazolyl group,

(4-38) a lower pyridyl alkanoyl group, (4-39) a thienylcarbonyl group, (4-40) a lower thienyl alkanoyl group, (4-41) a lower cycloalkyl alkanoyl group, (4-42) a isoxazolylcarbonyl group optionally substituted in

isoxazole ring with one or more lower alkyl groups, (4-43) a pyrazylcarbonyl group,

(4-44) a piperidinylcarbonyl group optionally substituted on the piperidine ring with one or more members selected from a benzoyl group and lower alkanoyl groups,

(4-45) a chromanylcarbonyl group,

(4-46) a lower isoindolinyl alkanoyl group optionally substituted on the isoindoline ring with one or more oxo groups,

(4-47) a thiazolidinyl lower alkanoyl group optionally substituted on the thiazolidine ring with one or more members selected from an oxo group and a thioxo group, (4-48) a piperidinyl lower alkanoyl group,

(4-49) a lower alkenylcarbonyl phenyl group optionally substituted on the phenyl ring with one or more halogen atoms,

(4-50) a phenyl substituted lower alkenylcarbonyl group at the phenyl level with one or more alkylenedioxy groups, (4-51) a pyridyl lower alkenylcarbonyl group,

(4-52) a lower alkanoyl pyridylthio group, (4-53) an indolylcarbonyl group, (4-54) a pyrrolylcarbonyl group,

(4-55) a pyrrolidinylcarbonyl group optionally substituted on the pyrrolidine ring with one or more oxo groups, (4-56) a benzofurylcarbonyl group, (4-57) a lower indolyl alkanoyl group, (4-58) a benzothienylcarbonyl group,

(4-59) a phenyl lower alkanoyl group optionally substituted on the phenyl ring with one or more halogen atoms,

(4-60) a phenylsulfonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxycarbonyl groups; a cyan group; a nitro group; optionally substituted nitro groups with one or more alkanoyl groups; a hydroxy group; a carboxyl group; lower alkyl lower alkoxycarbonyl groups; halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; and lower alkoxy groups optionally substituted with one or more halogen atoms,

(4-61) an optionally substituted thiosulfonyl group on the thiophene ring with one or more members selected from the group consisting of halogen atoms and lower alkoxycarbonyl groups, (4-62) an quinolylsulfonyl group, (4-63) an optionally substituted imidazolylsulfonyl group on the imidazole ring with one or more lower alkyl groups,

(4-64) an phenylsulfonyl group optionally substituted on the phenyl ring with one or more lower alkylenedioxy groups, (4-65) a lower alkenylsulfonyl group,

(4-66) a lower cycloalkyl alkylsulfonyl group, (4-67) an 3,4-dihydro-2H-1,4-benzoxazinylsulfonyl group optionally substituted on the 3,4-dihydro-2H-1,4-benzoxazine ring with one or more lower alkyl groups, (4-68) an optionally substituted pyrazolylsulfonyl group on the

pyrazole ring with one or more members selected from halogen atoms and lower alkyl groups,

(4-69) an isoxazolyl sulfonyl group optionally substituted on the isoxazole ring with one or more lower alkyl groups, (4-70) an optionally substituted thiazolyl sulfonyl group on the

triazole ring with one or more members selected from the group consisting of lower alkyl groups and one amino group, each amino substituent optionally being substituted with one or more alkanoyl groups, (4-71) one lower alkylsulfonyl group, (4- 72) a lower alkenylsulfonyl phenyl group,

(4-73) a naphthyloxycarbonyl group, (4-74) a lower alkynyloxycarbonyl group, (4-75) a lower alkenyloxycarbonyl group, (4-76) a lower alkoxycarbonyl group substituted by phenylalkyl

lower cab,

(4-77) a cycloalkyloxycarbonyl group optionally substituted on the cycloalkyl ring with one or more lower alkyl groups, (4-78) a tetrazolyl group,

(4-79) an isoxazolyl group optionally substituted on the isoxazole ring with one or more lower alkyl groups; or instead,

R 6 and R 7 may be bonded together to form, together with the nitrogen atom to which they are attached, a 1,2,3,4-tetrahydroisoquinolyl group, an isoindolinyl group, or a saturated 5 to 10 heterocyclic group. 7-membered, the heterocyclic group optionally containing one or more additional heteroatoms and optionally being substituted with one to three members of the following (5-1) to (5-28): (5-1) lower alkyl groups,

(5-2) lower alkoxy groups, (5-3) an oxo group, (5-4) a hydroxy group, (5-5) lower alkyl pyridyl groups, (5-6) phenyl groups optionally substituted on the phenyl ring with

one or more members selected from the group consisting of halogen atoms; lower alkoxy groups optionally substituted with one or more halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; a cyan group; and a hydroxy group, (5-7) alkylenedioxy-substituted lower alkyl phenyl groups

bottom,

(5-8) phenyl lower alkyl groups optionally substituted on the phenyl ring with one or more halogen atoms, (5-9) pyrimidyl groups, (5-10) pyrazyl groups,

(5-11) cycloalkyl groups,

(5-12) phenyl lower alkoxy groups optionally substituted on the phenyl ring having one or more halogen atoms,

(5-13) optionally substituted benzoyl groups on the phenyl ring having one or more halogen atoms,

(5-14) phenyl ring substituted benzoyl groups having one or more lower alkylenedioxy groups,

(5-15) lower alkylcarbamoyl groups optionally substituted by one or more members selected from the group consisting of a phenyl group and lower alkyl groups,

(5-16) benzoxazolyl groups, (5-17) lower alkoxycarbonyl groups, (5-18) a carbamoyl group,

(5-19) optionally substituted lower alkylidene phenyl groups on the phenyl ring having one or more halogen atoms, (5-20) lower alkoxycarbonyl phenyl groups, (5-21) optionally substituted pyridine ring pyridyl groups

with one or more members selected from the group consisting of a cyano group and lower alkyl groups,

(5-22) lower alkyl furyl groups, (5-23) tetrahydropyranyl groups, (5-24) imidazolyl lower alkyl groups,

(5-25) naphthyl groups, (5-26) 2,3-dihydro-1H-indenyl groups, (5-27) lower alkyl groups 1,3-dioxolanyl, (5-28) groups - (A3) mNR11R12; A1 is a lower alkylene group;

R 8 and R 9 each independently represent one of the following (6-1) to (6-25):

(6-1) a hydrogen atom, (6-2) a lower alkyl group, (6-3) a phenyl group optionally substituted on the phenyl ring

with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; lower alkylthio groups; lower alkoxy groups optionally substituted with one or more halogen atoms; halogen atoms; a phenyl group; mono-lower alkyl groups; a cyan group; a phenoxy group; cycloalkyl groups; pyrrolidinyl groups optionally substituted with one or more oxo groups; 1,2,3,4-tetrahydroisoquinolylcarbonyl groups; 1,2,3,4-tetrahydroquinolinylcarbonyl optionally substituted with one or more lower alkyl groups; 1,2,3,4-tetrahydroquinoxalinylcarbonyl groups optionally substituted by one or more lower alkyl groups; thiazolyl groups optionally substituted with one or more phenyl groups; a carbamoyl group; phenyl lower alkoxy groups; lower alkylsulfonylamino groups; optionally substituted anilino groups having one or more halogen atoms; phenyl lower alkyl groups; hydroxy-substituted lower alkyl groups, (6-4) a cycloalkyl group, (6-5) a lower cycloalkyl group, (6-6) a lower alkylcarbamoyl group,

(6-7) a lower alkyl phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups optionally substituted with one or more halogen atoms; halogen atoms; and a phenyl group,

(6-8) lower alkyl-substituted amino lower alkyl group, (6-9) a naphthyl group, (6-10) a lower alkyl naphthyl group, (6-11) a lower alkyl tetrahydronaphthyl group, (6-12) a fluorenyl group,

(6-13) a pyridyl group, (6-14) a lower alkyl pyridyl group, (6-15) a pyrimidinyl group,

(6-16) a lower alkyl pyrazinyl group optionally substituted on the pyrazine ring with one or more lower alkyl groups, (6-17) a thiazolyl group,

(6-18) a lower alkyl pyrazolyl group optionally substituted on the pyrazole ring with one or more lower alkyl groups, (6-19) a lower alkyl thienyl group (6-20) an optionally substituted piperidinyl group on the ring

piperidine with one or more members selected from the group consisting of lower alkyl group; a benzoyl group; and optionally substituted lower alkyl phenyl groups on the phenyl ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups, (6-21) an indolyl group,

(6-22) an indazolyl group,

(6-23) a 3,4-dihydrocarbostyril optionally substituted with one or more lower alkyl groups,

(6-24) a quinolyl group optionally substituted by one or more lower alkyl groups,

(6-25) a carbazolyl group optionally substituted with one or more lower alkyl groups; or

R 8 and R 9 may be bonded together to form, together with the nitrogen atom to which they are attached, a 5 or 8 membered saturated heterocyclic group optionally containing one or more additional heteroatoms and optionally substituted on the heterocyclic ring with one. or more selected members of the group consisting of the following (6-28-1) to (6-28-24):

(6-28-1) lower alkyl groups,

(6-28-2) optionally substituted lower alkyl phenyl groups on the phenyl ring having one or more members selected from halogen atoms and optionally substituted lower alkoxy groups with one or more halogen atoms,

(6-28-3) lower alkyl naphthyl groups, (6-28-4) lower alkylphenyl lower alkylcarbamoyl groups, (6-28-5) lower alkylphenylcarbamoyl groups, (6-28-6) lower alkoxycarbonyl phenyl groups,

(6-28-7) lower alkyl phenoxy groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, (6-28-8) biphenyl groups,

(6-28-9) optionally substituted phenyl groups on the phenyl ring having one or more halogen atoms,

(6-28-10) 2,3-dihydroindenyl groups optionally substituted with one or more halogen atoms, (6-28-11) optionally substituted benzothiazolyl groups

one or more halogen atoms,

(6-28-12) pyridyl groups optionally substituted by one or more halogen atoms,

(6-28-13) benzothienyl groups, (6-28-14) benzoisothiazolyl groups, (6-28-15) thienopyridyl groups, (6-28-16) a carbamoyl group,

(6-28-17) phenyl lower alkoxy groups optionally substituted on the phenyl ring having one or more halogen atoms,

(6-28-18) phenoxy groups optionally substituted with one or more halogen atoms,

(6-28-19) optionally substituted benzoyl groups on the phenyl ring with one or more members selected from halogen atoms and lower alkoxy groups,

(6-28-20) optionally substituted anilino groups on the phenyl ring having one or more lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more halogen atoms,

(6-28-21) amino group substituted on the amino group with one or more lower alkyl groups, and optionally also substituted on the phenyl ring with one or more halogen atoms, (6-28-22) benzofuryl groups, (6-28 -23) naphthyl groups, (6-28-24) an oxo group; or

R 8 and R 9 may be linked together to form, together with the nitrogen atom to which they are attached, a 5 or 6 membered unsaturated heterocyclic group, the unsaturated heterocyclic group optionally being substituted on the heterocyclic ring with one or more selected members of the group consisting of the following (6-29-1) to (6-29-3):

(6-29-1) phenyl groups optionally substituted by one or more halogen atoms,

(6-29-2) 2,3-dihydroindenyl groups,

(6-29-3) benzothienyl groups; or instead,

R 8 and R 9 may be bonded together to form, together with the nitrogen atom to which they are attached, a 1,2,3,4-tetrahydroquinolyl group; a 1,2,3,4-tetrahydroisoquinolyl group, a 1,3-dihydroisoindolyl group; an octahydropyrrol [1,2-a] pyrazinyl group optionally substituted on the pyrazine ring with one or more lower alkyl groups; or an 8-azabicyclo [3,2,1] octyl group optionally substituted on the 8-azabicyclo [3,2,1] octyl group with one or more phenoxy groups, each phenoxy substituent being optionally substituted on the phenyl ring with a or more halogen atoms;

A2 is a lower alkylene group; R10 is one of the following (7-1) to (7-44):

(7-1) a hydrogen atom, (7-2) a lower alkyl group,

(7-3) an alkoxycarbonyl group optionally substituted with one or more halogen atoms, (7-4) an optionally substituted benzoyl group on the phenyl ring

with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; a phenyl group; halogen atoms; a cyan group; a phoxy group; lower alkoxycarbonyl groups; pyrazolyl groups; and lower alkoxy groups optionally substituted with one or more halogen atoms, (7-5) an alkanoyl group,

(7-6) a lower phenyl alkanoyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups, (7-7) a lower cycloalkyl alkanoyl group,

(7-8) a phenyl group optionally substituted on the phenyl ring with one or more lower alkyl groups,

(7-9) a lower alkanoyl phenoxy group optionally substituted on the phenyl ring with one or more halogen atoms, (7-10) a lower alkenylcarbonyl phenyl group,

(7-11) a pyridylcarbonyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more halogen atoms,

(7-12) a furylcarbonyl group, (7-13) a thienylcarbonyl group,

(7-14) a piperidinylcarbonyl group optionally substituted on the piperidine ring with one or more lower alkanoyl groups,

(7-15) a pyrrolidinylcarbonyl group optionally substituted on the pyrrolidine ring with one or more oxo groups, (7-16) a tetrahydropyranylcarbonyl group,

(7-17) a naphthylcarbonyl group, (7-18) an indolylcarbonyl group, (7-19) a benzofurylcarbonyl group,

(7-20) a benzothienylcarbonyl group optionally substituted on the benzothiophene ring with one or more halogen atoms, (7-21) a lower alkyl furyl group,

(7-22) a lower alkyl pyridyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more carbon atoms. halogen,

(7-23) a thienyl lower alkyl group optionally substituted on the thiophene ring with one or more halogen atoms,

(7-24) a lower alkyl phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxy groups optionally substituted with one or more halogen atoms; a cyan group; lower alkyl groups optionally substituted with one or more halogen atoms; amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups; halogen atoms; lower alkoxycarbonyl groups; lower alkanoyloxy groups; lower alkylsulfonyl groups; lower alkylthio groups; and pyrrolidinyl groups, (7-25) a lower alkyl thiazolyl group,

(7-26) a lower alkyl imidazole group optionally substituted on the imidazole ring with one or more lower alkyl groups,

(7-27) a pyrrolyl lower alkyl group optionally substituted on the pyrrol ring with one or more lower alkyl groups, (7-28) a lower cycloalkyl alkyl group, (7-29) a lower alkyl lower alkyl group, (7 -30) a phenoxycarbonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms, lower alkyl groups, and lower alkoxy groups,

(7-31) a lower phenyl alkoxycarbonyl group optionally substituted on the phenyl ring with one or more halogen atoms, (7-32) a naphthyloxycarbonyl group, (7-33) a lower alkynyloxycarbonyl group, (7-34) a cycloalkylcarbonyl group ,

(7-35) a quinoxalinylcarbonyl group, (7-36) a -CO-NR 13 R 14 group,

(7-37) a piperidinyl group optionally substituted on the piperidine ring with one or more lower alkyl groups, (7-38) a cycloalkyl group,

(7-39) a tetrahydropyranyl group, (7-40) a lower alkyl lower alkoxy group, (7-41) a tetrahydro-2H-thiopyranyl group, (7-42) a naphthyl group, (7-43) a group biphenyl,

(7-44) a lower alkoxycarbonyl group lower alkylsilyl; A3 is a lower alkylene group; m is 0 or 1;

R 11 and R 12 each independently represent one of the following (8-1) to (8-5):

(8-1) a hydrogen atom, (8-2) a lower alkyl group, (8-3) a lower alkanoyl group,

(8-4) a lower phenyl alkanoyl group,

(8-5) a phenyl group optionally substituted on the phenyl ring with one or more halogen atoms; or instead, R11 and R12 may be linked together to form together

with the nitrogen atom to which they are attached, a 5- or 6-membered saturated heterocyclic group optionally containing one or more additional hetero atoms, the heterocyclic group optionally being substituted with one to three members selected from the group consisting of the following (9). -1) and (9-2):

(9-1) lower alkyl groups,

(9-2) a phenyl group; and

R 13 and R 14 each independently represent one of the following (10-1) to (10-3): (10-1) a hydrogen atom,

(10-2) a lower alkyl group,

(10-3) a phenyl group, or instead

R13 and R14 may be bonded together to form, together with the nitrogen atom to which they are attached, a 5- or 6-membered saturated heterocyclic group which optionally contains one or more additional hetero atoms.

2. The agent according to item 1 wherein the disease associated with NF-κΒ is selected from the group consisting of reperfusion disorders in ischemic diseases, exacerbation of organ transplantation prognosis.

organ surgery or surgery, post-PTCA restenosis, cancer invasion and metastasis, and cachexia.

3. The agent according to item 1, which is to regulate the transcription of cytokines and / or adherence factors.

4. The agent according to item 3, which is to inhibit the activity of COX-2, TNF-oc, and / or IL-8.

5. A preventive or therapeutic agent for a COX-2 associated disorder or disease comprising the carbostyril compound of item 1 or a salt thereof as an active ingredient.

6. An anticancer effect enhancer for use in radiotherapy or chemotherapy comprising the carbostyril compound of item 1 or a salt thereof as an active ingredient.

7. A radiosensitivity enhancer for use in radiotherapy

comprising the carbostyril compound of item 1 or a salt thereof as an active ingredient.

8. A tumor-induced angiogenesis inhibitor comprising the carbostyril compound of item 1 or a salt thereof as an ingredient.

active patient.

A method for enhancing anticancer effects in radiotherapy or chemotherapy, comprising administering an effective amount of the carbostyril compound of item 1 or a salt thereof to a patient.

10. Use of the carbostyril compound of item 1 or a salt thereof

to boost the anticancer effect for use in radiotherapy or

chemotherapy.

The agent according to item 1, wherein the carbostyril compound is represented by General Formula (1) wherein R 4 and R 5 each represent a hydrogen atom.

12. The agent according to item 11, wherein the compound of

carbostyril is represented by General Formula (1) wherein a group of Formula

R \ .o

wherein R3, A and X are as defined in item 1 above, is attached to position 3, 4, 5, 6, 7 or 8 of the carbostyril backbone.

13. The agent according to item 12, wherein the compound of

Carbostyryl is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a single bond, and the group of Formula, R 1,

χ

s

wherein R31 A and X are as defined in item 1 above, is attached to position 5 or 6 of the carbostyril backbone.

14. The agent of item 12 or 13, wherein the carbostyril compound is represented by General Formula (1) wherein A is a

lower alkylene or lower alkylidene group.

15. The agent of item 14, wherein the carbostyril compound is represented by General Formula (1) wherein R1 is one of (1-2), (1-3), (1-4), ( , .β), (1-10), (1-12), (1-13), (1-18) and (1-21) as defined in item 1 above.

16. The agent according to item 15, wherein the compound of

carbostyril is represented by the general formula (1) in which the group of Formula

River

x S

wherein R3, A and X are as defined in item 1 above, is attached to position 5 of the carbostyril backbone.

17. The agent according to item 16, wherein the compound of

Carbostyryl is represented by General Formula (1) wherein R1 is a lower alkyl phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of a phenyl ring, halogen atoms, groups - (B), NR6R7 wherein Β, I, R6 and R7 are as defined in

item 1, lower alkoxycarbonyl groups and phenyl lower alkoxy groups.

18. The agent according to item 17 wherein the carbostyril compound is represented by General Formula (1) wherein A is a lower alkylene group, R2 is a hydrogen atom or a lower alkoxy group, R3 is a hydrogen atom, and X is an oxygen atom or a hydrogen atom.

sulfur.

19. The agent according to item 16 wherein the carbostyril compound is represented by General Formula (1) wherein A is a lower alkylene group, R1 is a lower alkyl group, R2 is a hydrogen atom or a lower alkoxy group, R3 is a hydrogen atom, and X is an oxygen atom or a sulfur atom.

20. The agent of item 16, wherein the carbostyril compound is represented by General Formula (1) wherein A is an alkenyl group.

lower kilene, R1 is a lower alkyl naphthyl group, R2 is a hydrogen atom or a lower alkoxy group, R3 is a hydrogen atom, and X is an oxygen atom or a sulfur atom.

21. The agent according to item 16, wherein the carbostyril compound is represented by General Formula (1) wherein A is an alkenyl group.

lower kilene, R1 is a group of Formula

2 \ *

-NA-R10

wherein R10 and A2 are as defined in item 1 above, R2 is a hydrogen atom or a lower alkoxy group, R3 is a hydrogen atom, and X is an oxygen atom or a sulfur atom. 22. The agent according to item 12, wherein the compound of

carbostyril is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a double bond, and a group of Formula

R3x Λ0

wherein R3, A and X are as defined in item 1 above, is attached to position 3, 4 or 5 of the carbostyril backbone.

23. The agent according to item 22, wherein the carbostyril compound is represented by General Formula (1) wherein R1 is one of (1-2) and (1-3) as defined in item 1.

24. The agent of item 23, wherein the carbostyril compound is represented by General Formula (1) wherein A is an alkenyl group.

lower kilene or lower alkydylene group, and R2 is a hydrogen atom or lower alkoxy group. 25. The agent of item 1, wherein the carbostyril compound is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a double bond, and R 4 and R 5 are bonded. together as a group -CH = CH-CH = CH-.

26. The agent of item 25, wherein the carbostyril compound is represented by General Formula (1) wherein a group of Formula

Laugh

X s

wherein R3, A and X are as defined in item 1 above, is attached to position 7 of the carbostyril backbone.

27. The agent according to item 26, wherein the compound of

Carbostyryl is represented by General Formula (1) wherein R1 is one of (1-2) and (1-3) as defined in item 1 above.

28. The agent of item 27, wherein the carbostyril compound is represented by General Formula (1) wherein A is an alkenyl group.

lower kilene or lower alkylidene group, R2 and R3 are both hydrogen atoms, and X is an oxygen atom or a sulfur atom.

29. The agent according to item 1, wherein the carbostyril compound is represented by General Formula (1) wherein A is a direct bond.

30. The agent according to item 1, wherein the compound of

Carbostyril is represented by General Formula (1) wherein A is a lower alkylene group.

31. The agent according to item 1, wherein the carbostyril compound is represented by General Formula (1) wherein A is an alkenyl group.

lower kilidene.

32. The agent according to any of items 29 to 31, wherein the carbostyril compound is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a single or a double bond, and R4 and R5 each represent an

hydrogen atom. 33. The agent of any of items 29 to 31, wherein the carbostyril compound is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a double bond, and R4 and R5 are joined together as a group -

CH = CH-CH = CH-.

34. The agent according to item 1, wherein the carbostyril compound is selected from the group consisting of the following compounds: 5- [1- (biphenyl-4-ylmethyl) -8-methoxy-2-oxo-1,2 3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- [1- (4-chlorobenzyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- [1- (4-bromobenzyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- [1- (2-naphthylmethyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- {1- [4- (heptyloxycarbonylamino) benzyl] -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione,

5- [1- (1-biphenyl-4-ylpiperidin-4-ylmethyl) -2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- {1- [1- (4-methylphenyl) piperidin-4-ylmethyl] -2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione,

5- {1- [4- (2-chlorobenzyloxycarbonylamino) benzyl] -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione,

1- (biphenyl-4-ylmethyl) -8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

8-methoxy-1-methyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

8-methoxy-1- (3-methylbutyl) -5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

1-propyl-8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

1-Isobutyl-8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

8-Methoxy-1-phenethyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one, and

1- (4-phenylthiomethyl) benzyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one; or a salt of these. Carbostyril Compounds

Carbostyryl compounds represented by General Formula (1) used in the present invention are known compounds, and described, for example, in WO2006 / 035954. Specific examples of groups in the above General Formula (1) are

as follows.

Examples of lower alkylene groups include straight or branched C1-6 alkylene groups such as methylene, ethylene, trimethylene, 2-methyltrimethylene, 2,2-dimethylethylene, 2,2-dimethyltrimethylene, 1-methyltrimethylene, methylmethylene ethyl ethylene, tetramethylene, pentamethylene, and hexamethylene.

Examples of lower alkylene groups include straight and branched C 1-6 alkylidene groups such as methylidene, ethylidene, propylidene, butylidene, pentylidene, and hexylidene.

Examples of lower alkyl groups include straight or branched C1-6 alkyl groups such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, tert-butyl, sec-butyl, n-pentyl, isopentyl, neopentyl, n -hexyl, isoexyl, and 3-methylpentyl.

Examples of lower alkoxy groups include straight and branched C1-6 alkoxy groups such as methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, tert-butoxy, sec-butoxy, n-pentyloxy, isopentyloxy, neopentyloxy , n-hexyloxy, isoexyloxy, and 3-methylpentyloxy.

Examples of halogen atoms include fluorine, chlorine, bromine, and

iodine.

Examples of lower alkoxycarbonyl groups include alkoxycarbonyl groups wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group such as methoxycarbonyl, ethoxycarbonyl, n-propoxycarbonyl, isopropoxycarbonyl, n-butoxycarbonyl, isobutoxycarbonyl, butoxycarbonyl, sec-butoxycarbonyl, n-pentyloxycarbonyl, neopentyloxycarbonyl, n-hexyloxycarbonyl, isoexyloxycarbonyl, and 3-methylpentyloxycarbonyl.

Examples of phenyl lower alkoxy groups include phenylalkoxy groups wherein the alkoxy moiety is a branched or straight C1-6 alkoxy group such as benzyloxy, 2-phenylethyloxy, 1-phenylethyloxy, 3-phenylpropoxy, 4-phenylbutoxy, 5-phenylpentyloxy , 6-phenylexyloxy, 1,1-dimethyl-2-phenylethyloxy, and 2-methyl-3-phenylpropoxy.

Examples of lower alkoxycarbonyl piperidyl groups include piperidinylalkoxycarbonyl groups wherein the alkoxy moiety is a branched or straight C1-6 alkoxy group such as [(1-, 2-, 3-, or 4-) piperidinylmethoxycarbonyl, 2-

[(1-, 2-, 3-, or 4-) piperidinyl] ethoxycarbonyl, 1- [(1-, 2-, 3-, or 4-) piperidinyl] ethoxycarbonyl, 3- [(1-, 2-, 3-, or 4-) piperidinyl] propoxycarbonyl, A - [(1-, 2-, 3-, or 4-) piperidinyl] butoxycarbonyl, 5- [(1-, 2-, 3-, or 4-) piperidinyl ] pentyloxycarbonyl, 6-

[(1-, 2-, 3-, or 4-) piperidinyl] hexyloxycarbonyl, 1,1-dimethyl-2 - [(1-, 2-, 3-, or 4-) piperidinyl] ethoxycarbonyl, and 2-methyl -3 - [(1-, 2-, 3-, or 4-) piperidinyl] propoxycarbonyl.

Examples of cycloalkyl groups include C3-8 cycloalkyl groups such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloeptyl, and cyclooctyl.

Examples of lower alkoxycarbonyl amino groups optionally substituted with one or more alkyl groups include: amino substituted alkoxycarbonyl groups wherein the alkoxy moiety is a branched or straight C1-6 alkoxy group, optionally substituted with one or two C3-8 groups cycloalkyl;

such as aminomethoxycarbonyl, 2-aminoethoxycarbonyl, cyclopropylaminomethoxycarbonyl, 2-cyclohexylaminoethoxycarbonyl, 1-cyclobutylaminoethoxycarbonyl, 3-cyclopentylaminopropoxycarbonyl, 4-cycloheptylamobutylcarboxylamino-2-cyclohexylcarbonyl, cyclohexylaminoethoxycarbonyl, 2-methyl-3-cyclopropylaminopropoxycarbonyl, and 2- (N-cyclopropyl- V-cyclohexylamino) ethoxycarbonyl. Examples of lower alkylthio groups include straight and branched C1-6 alkylthio groups such as methylthio, ethylthio, n-propylthio, isopropylthio, n-butylthio, tert-butylthio, n-pentylthio, and n-hexylthio.

Examples of 2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring with one or more alkylthio groups include 2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring having one to three lower alkylthio groups, such as (1-, 2 -, 4-, or 5-) 2-imidazolinylcarbonyl,

2-methylthio- (1-, 4-, or 5-) 2-imidazolinylcarbonyl, 2-ethylthio- (1-, 4-, or 5-) 2-imidazolinylcarbonyl,

3-pyrroline ring acids with one or more lower alkyl groups include 3-pyrrolinylcarbonyl groups optionally substituted on the 3-pyrroline ring with one to three lower alkyl groups, such as (1-, 2-, or 3-) 3- pyrrolinylcarbonyl,

15

4-propylthio (1-, 2-, or 5-) 2-imidazolinylcarbonyl,

5-Isopropylthio- (1-, 2-, or 4-) 2-imidazolinylcarbonyl, 2-n-butylthio- (1-, 4-, or 5-) 2-imidazolinylcarbonyl, 2-n-pentylthio- (1-, 4-, or 5-) 2-imidazolinylcarbonyl, 2-n-hexylthio- (1-, 4-, or 5-) 2-imidazolinylcarbonyl, 2,4-dimethylthio- (1- or 5-) 2-imidazolinylcarbonyl, and 2,4,5-trimethylthio (1-) 2-imidazolinylcarbonyl.

Examples of optionally substituted 3-pyrrolinylcarbonyl groups

30

25

2-methyl- (1-, 2-, 3-, 4-, or 5-) 3-pyrrolinylcarbonyl,

2-ethyl- (1-, 2-, 3-, 4-, or 5-) 3-pyrrolinylcarbonyl,

3-propyl- (1-, 2-, 4-, or 5-) 3-pyrrolinylcarbonyl,

4-isopropyl- (1-, 2-, 3-, or 5-) 3-pyrrolinylcarbonyl,

5-n-butyl- (1-, 2-, 3-, 4-, or 5-) 3-pyrrolinylcarbonyl, 2- n-pentyl- (1-, 2-, 3-, 4-, or 5-) 3-pyrrolinylcarbonyl, 2-n-hexyl- (1-, 2-, 3-, 4-, or 5-) 3-pyrrolinylcarbonyl, 2,5-dimethyl- (1-, 2-, 3-, 4-, or 5-) 3-pyrrolinylcarbonyl, 2,4-dimethyl- (1-, 2-, 3-, or 5-) 3-pyrrolinylcarbonyl,

2,3-dimethyl- (1-, 2-, 4-, or 5-) 3-pyrrolinylcarbonyl, and 2,4,5-trimethylthio- (1-, 2-, 3-, or 5-) 3-pyrrolinylcarbonyl . Exemplary thiazolidinylcarbonyl groups optionally substituted on the thiazolidine ring with a phenyl group include (2-, 3-, 4-, or 5-) thiazolidinylcarbonyl,

2-phenyl- (3- '4-, or 5-) thiazolidinylcarbonyl, 3-phenyl- (2-, 4-, or 5-) thiazolidinylcarbonyl,

4-phenyl- (2- '3-, or 5-) thiazolidinylcarbonyl, and

5-phenyl- (2- ， 3-, or 4-) thiazolidinylcarbonyl.

Examples of lower alkylpiperidinyl groups include piperidinylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as [(1-, 2-, 3-, or 4-) piperidinyl] methyl,

2 - [(1- '' 2-, 3-, or 4-) piperidinyl] ethyl,

1 - [(1- '' 2-, 3-, or 4-) piperidinyl] ethyl,

3 - [(1-, 2-, 3-, or 4-) piperidinyl] propyl,

4 - [(1- '' 2-, 3-, or 4-) piperidinyl] butyl, 5 - [(1-, 2-, 3-, or 4-) piperidinyl] pentyl,

6 - [(1- '' 2-, 3-, or 4-) piperidinyl] hexyl,

1,1-dimethyl-2 - [(1-, 2-, 3-, or 4-) piperidinyl] ethyl, and

2-methyl-3 - [(1-, 2-, 3-, or 4-) piperidinyl] propyl.

Examples of lower alkyl anilino groups optionally substituted on the amino group with one or more lower alkyl groups include anilinoalkyl groups optionally substituted on the amino group with one or more C1-6 straight and / or branched alkyl groups, such as anilinomethyl, N - methylanilinomethyl, N-ethylanilinomethyl, N-n-propylanilinomethyl, N-isopropylanilomethyl, N-butylanilinomethyl, N-sec-butylanilinomethyl, N-n-butylanylmethyl, N / N-pentylanilomethyl N-hexylanilinomethyl, 2-anilinoethyl, 2- (N-methylanilino) ethyl, 2- (N-ethylanilino) ethyl, 2- (N-propylanilino) ethyl, 2- (N-isopropylanilino) ethyl, 2- (N-butylanilino) ethyl, 2- (N-sec-butylanilino) ethyl, 2- (N-butylanilino) ethyl, 2- (n-pentylanilino) ethyl, 2 - (N-N-hexylanilino) ethyl, 3-anilinopropyl, 3- (N-methylanilino) propyl, 4- (N-ethylanilino) butyl, 4- (N-propylanilino) butyl, 5 - (/ V- isopropylanilino) pentyl, 5- (N-butylanilino) pentyl, 6- (N-sec-butylanilino) h exyl, 6- (N-tert-butylanilino) hexyl, 6- (N-pentylanilino) hexyl, and 6- (N-hexylanilino) hexyl. Examples of lower phenylthioalkyl groups include phenylthioalkyl groups wherein the alkyl moiety is a straight or branched Cv6 alkyl group such as phenylthiomethyl, 2-phenylthioethyl, 1-phenylthioethyl, 3-phenylthiopropyl, 4-phenylthiobutyl, phenylthiopentyl, 6-phenylthiohexyl, 1,1-dimethyl-2-phenylthioethyl, and 2-methyl-3-phenylthiopropyl.

Examples of indolinyl lower alkyl groups include Indo-ynylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, such as

[(1-, 2- 3-, 4-, 5-, 6-, DU 7-) indolinyl] methyl, 2 - [(1- '2-, 3-, 4-, or 5-) indolinyl] ethyl, 1 - [(1-, 2-, 3-, 4-, 5-, 6 · ■ ， or 7) indolinyl] ethyl, 3 - [(1-, 2-, 3-, 4-, 5- , 6- ·, or 7) indolinyl] propyl, 4 - [(1- '2-, 3-, 4-, 5-, 6- ， or 7) indolinyl] butyl, 5 - [(1-, 2- , 3-, 4-, 5-, 6-, or 7) indolinyl] pentyl, 6 - [(1- '2-, 3-, 4-, 5-, 6-, or 7) indolinyl] hexyl, 1 , 1-dimethyl-2 ■ [(1 - ， 2-, 3-, 4-, 5-, 6-, or 7) indolinyl] ethyl, and 2

[(1-, 2-, 3-, 4-, 5-, 6-, or 7) indolinyl] propyl.

Examples of optionally substituted piperidinylcarbonyl groups on the piperidine ring with one or more lower alkyl groups include piperidinylcarbonyl groups optionally substituted on the piperidine ring with one to three linear and / or branched C1-6 alkyl groups, such as (1-, 2 -, 3-, or 4-) piperidinylcarbonyl, 1-methyl- (2-, 3-, or 4-) piperidinylcarbonyl, 1-ethyl- (2-, 3-, or 4-) piperidinylcarbonyl, 1-n-propyl - (2-, 3-, or 4-) piperidinylcarbonyl, 1-n-butyl- (2- '3-, or 4-) piperidinylcarbonyl, 1-n-pentyl- (2-, 3-, or 4-) piperidinylcarbonyl'-n-hexyl- (2- '3-, or 4-) piperidinylcarbonyl, 1,2'-dimethyl- (3-, 4-, 5-, or 6-) piperidinylcarbonyl, 1,2,3 -trimethyl- (4-, 5-, or 6-) piperidinylcarbonyl, 2-β-propyl- (1-, 3-, 4-, 5-, or 6-) piperidinylcarbonyl, 3-ethyl- (1-, 2-, 4-, 5-, or 6-) piperidinylcarbonyl and 2-methyl-4-isopropyl- (1-, 3-, 5-, or 6-) piperidinylcarbonyl.

Examples of optionally substituted lower alkyl phenyl groups on the phenyl ring with one or more members selected from the group consisting of a phenyl group; lower alkyl groups; lower alkoxy groups; halogen atoms; groups - (B) | NR6R7; a nitro group; a carboxy group; lower alkoxycarbonyl groups; a cyan group; phenyl lower alkoxy groups; a phenoxy group; piperidinyl lower alkoxycarbonyl groups; lower alkoxycarbonyl amino groups optionally substituted by one or more cycloalkyl groups; 2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring with one or more lower alkylthio groups; 3-pyrrolinylcarbonyl groups optionally substituted on the pyrrol ring with one or more lower alkyl groups; thiazoldinylcarbonyl groups optionally substituted on the thiazolidine ring with a phenyl group; 3-azabicyclo [3'2,2] nonylcarbonyl groups; piperidinyl lower alkyl groups; optionally substituted lower alkyl anilyl groups on the amino group with one or more lower alkyl groups; phenyl lower alkyl groups; indolinyl lower alkyl groups; and optionally substituted piperidinylcarbonyl groups on the piperidine ring with one or more lower alkyl groups include:

mono- and di-phenylalkyl groups wherein the alkyl moiety is a branched or branched C1-6 alkyl group, optionally substituted on the phenyl ring with one to three members selected from the group consisting of a phenyl group; the linear and branched C1 -C4 alkyl groups described above; the linear and branched C1-6 alkoxy groups described above; halogen atoms; the (B) NR6 R7 groups described above; a nitro group; a carboxy group; the linear and branched C1-6 alkoxycarbonyl groups described above; a cyan group; phenylalkoxy groups described above wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group; a phenoxy group; the piperidinylalkoxycarbonyl groups described above wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group; the aminoalkoxycarbonyl groups described above wherein the alkoxy moiety is a straight or branched C6 alkoxy group optionally substituted with one or two C3.8 cycloalkyl groups; the above-described 2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring with one to three linear and / or branched C1-6 alkylthio groups; the above-described 3-pyrrolinylcarbonyl groups optionally substituted on the 3-pyrroline ring having one to three linear and / or branched C1-6 alkyl groups; optionally substituted thiazolidinylcarbonyl groups on the ring

thiazolidine with a phenyl group; 3-azabicyclo [3，2'2] nonylcarbonyl groups; piperidinylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group; anilinoalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the amino group with one or two straight and / or branched C1-6 alkyl groups; phenylthioalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group; indolinylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group; and the above-described piperidinylcarbonyl groups optionally substituted on the piperidine ring with one to three linear and branched C 1-6 alkyl groups; such as benzyl, 1-phenethyl, 2-phenethyl, 3-phenylpropyl, 2-phenylpropyl

4-phenylbutyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenylexyl, 2-methyl-3-phenylpropyl, 1,1-dimethyl-2-phenylethyl, 1,1-diphenylmethyl, 2,2-diphenylethyl, 3,3-diphenylpropyl, 1,2-diphenylethyl, 4- [N- (3-pyridyl) aminocarbonyl] benzyl, 4- [N- (2-methoxyphenyl) aminocarbonyl] benzyl, 4- [2- ( 2-piperidinyl) ethoxycarbonyl] benzyl,

4- [2- (cyclohexylamino) ethoxycarbonyl] benzyl, 4- [4- (3-pyridylmethyl) -1-piperazinylcarbonyl] benzyl, 4- [4- (4-pyridylmethyl) -1-piperazinylcarbonyl] benzyl, 4- [4 - (2-pyridylmethyl) -1-piperazinylcarbonyl] benzyl, 4- [4- (2-pyridyl) -1-piperazinylcarbonyl] benzyl,

4- [4- (3-chlorophenyl) -1-piperazinylcarbonyl] benzyl, 4- [4- (2-fluorophenyl) -1-piperazinylcarbonyl] benzyl, 4- [4- (2-pyrimidyl) -1-piperazinylcarbonyl] benzyl 4- (4-cyclopentyl-1-piperazinylcarbonyl) benzyl, 4- [4- (2-methoxyphenyl) -1-piperazinylcarbonyl] benzyl,

4- [4- (4-fluorophenyl) -1-piperazinylcarbonyl] benzyl, 4- [4- (3,4-methylenedioxybenzyl) -1-piperazinylcarbonyl] benzyl, 4- (N-cyclohexyl-Î ± -methylaminocarbonyl) benzyl ,

4- (N, N-di-n-butylaminocarbonyl) benzyl, 4- [4- (1-piperidinyl) -1-piperidinylcarbonyl] benzyl,

4- (1-homopiperidinylcarbonyl) benzyl,

4- [2-methylthio-1- (2-imidazolinyl) carbonyl] benzyl, 4- {N / - [2- (2-pyridyl) ethyl] - [N-methylaminocarbonyl} benzyl, 4- [[] / (( 1-methyl-4-piperidinyl) -Î ± -methylaminocarbonyl] benzyl,

4 - (/ V, A / -diisobutylaminocarbonyl) benzyl,

4 - [[V- (2-tetrahydropyranyl) methyl] [V-ethylaminocarbonyl] benzyl,

4- (4-thiomorpholinocarbonyl) benzyl,

4- [2'5-dimethyl-1- (3-pyrronyl) carbonyl] benzyl,

4- (3-thiazolidinylcarbonyl) benzyl,

4- (N-cyclopropylmethyl-N-n-propylaminocarbonyl) benzyl,

4- [1- (3-azabicyclo [3,2,2] nonylcarbonyl) benzyl,

4- (V-cyclopentyl- V-allylaminocarbonyl) benzyl,

4- [4- (4-pyridyl) -1-piperazinylcarbonyl] benzyl,

4- [4- (4-trifluoromethylphenyl) -1-piperazinylcarbonyl] benzyl,

4- [4- (2-phenylethyl) -1-piperazinylcarbonyl] benzyl,

4- [4- (2-pyrazyl) -1-piperazinylcarbonyl] benzyl,

4- (A / -A7-butylaminocarbonyl) benzyl,

4- (N-cyclopropylaminocarbonyl) benzyl,

4- [β / - (1-methyl-1-phenylethyl) aminocarbonyl] benzyl,

4- (V-benzylaminocarbonyl) benzyl,

4 - [[V- (2-chlorobenzyl) aminocarbonyl] benzyl,

4 - [[V- (3-chlorobenzyl) aminocarbonyl] benzyl,

4- [A / - (4-chlorobenzyl) aminocarbonyl] benzyl,

4- [A / - (2-pyridyl) methylaminocarbonyl] benzyl,

4- [A / - (3-pyridyl) methylaminocarbonyl] benzyl,

4 - [(4-pyridyl) methylaminocarbonyl] benzyl,

4- [3'5-dimethyl-1-piperidinylcarbonyl] benzyl,

4- [A / - (2-furyl) methylaminocarbonyl] benzyl,

4- [4- (2-fluorobenzyloxy) -1-piperidinylcarbonyl] benzyl,

4- {4- [N - (2-phenylacetyl) - [N-methylamino] -1-piperidinylcarbonyl} benzyl,

4 - [(4-methoxy-1-piperidinyl) carbonyl] benzyl,

4 - {[4- (3,4-dimethyl-1-piperazinyl) -1-piperidinyl] carbonyl} benzyl,

4 - {[4- (4-chlorobenzoyl) -1-piperidinyl] carbonyl} benzyl,

4 - {[4- (4-chlorobenzyl) -1-piperidinyl] carbonyl} benzyl, 4 - [(4-ethylcarbamoylmethyl-1-piperidinyl) carbonyl] benzyl, 4 - [(4-cyclohexyl-1-piperidinyl) carbonyl] benzyl, 4 - {[4- (4-methoxyphenyl) -1-piperidinyl] carbonyl} benzyl, 4 - {[4- (2-benzoxazolyl) -1-piperazinyl] carbonyl} benzyl, 4 - [(4-anilinocarbonylmethyl-1 - piperazinyl) carbonyl] benzyl, 4 - [(4-methyl-2-benzyl-piperazinyl) carbonyl] benzyl, 4 - [(4-phenyl-3-oxo-1-piperazinyl) carbonyl] benzyl, 4 - [(4-merceryl) butyl-3-oxo-1-piperazinyl) carbonyl] benzyl, 4- [[V- (1-benzoyl-4-piperidinyl) - [N-methylaminocarbonyl] benzyl] 4- [N (1-acetyl-4-piperidinyl) -A / -methylaminocarbonyl] benzyl,

4 - {[4- (4-cyanophenyl) -1-piperazinyl] carbonyl} benzyl, 4 - [/ V-methylcarbamoylmethyl-A / -benzylaminocarbonyl] benzyl ， 4 - [/ V-benzyl- / V-cyclohexylaminocarbonyl] benzyl, 4- [2- (N-methyl- [N-phenylcarbamoyl) ethyl] N-methylaminocarbonyl] benzyl, 4 - {[4- (3-phenyl-1-pyrrolidinyl) -1-piperidinyl] carbonyl} benzyl, 4 - [(1,2,3,4 tetrahydroisoquinoline-2-yl) carbonyl] benzyl,

4 - [(4-benzyl-1-piperidinyl) carbonyl] benzyl, 4 - {[4- (3,4-methylenedioxybenzoyl) -1-piperazinyl] carbonyl} benzyl,

4 - [[V-methyl- [V- (4-methylbenzyl) aminocarbonyl] benzyl, 4- [Î ± -methyl - [[- (3,4-methylenedioxybenzyl) aminocarbonyl] benzyl, 4 [[V-methylmethyl] [2- (2-Methoxybenzyl) aminocarbonyl] benzyl, 4 - [(4-phenyl-1-piperazinyl) carbonyl] benzyl, 4 - [(4-phenyl-4-hydroxy-1-piperidinyl) carbonyl] benzyl, 4- (N-isopropyl) -A (-benzylaminocarbonyl) benzyl, 4- ([/] ethyl- [N -cyclohexylaminocarbonyl) benzyl, 4- [A] -ethyl-A / - (4-pyriclyl) methylaminocarbonyl] benzyl, 4 - (/ Vn- propylaminocarbonyl) benzyl, 4- [Î ± -ethyl- [[- (4-ethoxybenzyl) aminocarbonyl] benzyl, 4- (Î ± -ethyl- [Î ± -cyclohexylmethylaminocarbonyl) benzyl, 4- [β- (2-ethoxyethyl) ) aminocarbonyl] benzyl, 4- [N / - (1,1-dimethyl-2-phenylethyl) aminocarbonyl] benzyl, 4 - [{4- [N-methyl- [N- (4-chlorophenyl) amino] -1 -piperidinylcarbonyl] benzyl 4- [β- - (1-methyl-1-cyclopentyl) aminocarbonyl] benzyl, 4 - [/ V- (1-methyl-1-cycloexyl) aminocarbonyl] benzyl, 4 - {/ V- [2 - (3-methoxyphenyl) ethyl] aminocarbonyl} benzyl, 4- [N / - (4-trifluoromethoxybenzyl) aminocarbonyl] benzyl, 4 - {/ V- [2- (4-chlorophenyl) ethyl] aminoc arbonyl} benzyl, 4 - [[V- (3,4-methylenedioxybenzyl) aminocarbonyl] benzyl, 4- (V-cyclohexylmethylaminocarbonyl) benzyl, 4- [N / - (4-fluorobenzyl) aminocarbonyl] benzyl, 4- [A / - (1 -phenylethyl) aminocarbonyl] benzyl, 4 - [[V- (3-phenylpropyl) aminocarbonyl] benzyl, 4 - {/ V- [3- (1-imidazolyl) propyl] aminocarbonyl} benzyl, 4 - [/ V- (2-phenylethyl) aminocarbonyl ] benzyl, 4- [2- (N-, [N-diisopropylamino) ethylaminocarbonyl] benzyl, 4- {N / - [1-methoxycarbonyl-2- (4-hydroxyphenyl) ethyl] aminocarbonyl} benzyl

over there,

4 - [[V- (carbamoylmethyl) aminocarbonyl] benzyl, 4- {Î ± - [1-carbamoyl-2- (5-imidazolyl) ethyl] aminocarbonyl} benzyl, 4 {[V- [1-methoxycarbonyl-2- (5- imidazo）） ethyl] amino carbonyljbenzyl, 4- [Λ / - (2-οχο 2,3,4,5-tetrahydrofuran-3-yl) aminocarbonyljbenzyl,

4 - [(2-ethoxycarbonyl-1-piperidinyl) carbonyl] benzyl, 4- (N-methoxycarbonylmethyl-N-methylaminocarbonyl) benzyl, 4 - [(2-carbamoyl-1-pyrrolidinyl) carbonyl] benzyl, 4- { [? / - (2,6-dimethylbenzyl) - [Î ± -ethyl] aminocarbonyl} benzyl, 4- {Î ± - [(4-methylphenyl) carbamoylmethyl] -β-methylaminocarbonyl} benzyl 4 - [/ V- (4-chlorobenzyl) - / V-ethylaminocarbonyl] benzyl, 4 - [/ V- (4-trifluoromethylbenzyl) - / V-ethylaminocarbonyl] benzyl, 4- [A / - (3-bromobenzyl) - / V * ethylaminocarbonyl] benzyl , 4 - {[4- (2-chlorobenzyl) -1-piperidinyl] carbonyl} benzyl, 4 - {[4- (3-chlorobenzyl) -1-piperidinyl] carbonyl} benzyl, 4 - {[4- (2- chlorobenzylidene) -1-piperidinyl] carbonyl} benzyl, 4- [A / - (2-methoxybenzyl) aminocarbonyl] benzyl, 4- {A / - [2- (2-fluorophenyl) ethyl] aminocarbonyl} benzyl, 4 - {/ V- [2- (3-fluorophenyl) ethyl] aminocarbonyl} benzyl, 4 - [(4-benzyloxycarbonyl-1-piperazinyl) carbonyl] benzyl, 4 - {[4- (3-cyano-2-pyridyl) -1-piperazinyl] carbonyl} benzyl, 4 - [(4-phenyl-1-piperidinyl) carbonyl] benzyl, 4 - [{4 - [(3-furyl) methyl] -1-piperazinyl} carbonyl] benzyl, 4- {[4- (3-pyridyl) -1-piperazinyl] carbonyl} benzyl, 4 - {[4- (4-tetrahydropyranyl) -1-piperazinyl] carbonyl} benzyl, 4 - {[4- (2-fluorobenzyl) - 1-piperidinyl] carbonyl} benzyl, 4 - {[4- (4-morpholino) -1-piperidinyl] carbonyl} benzyl, 4- {4- [2- (1，3-dioxolane-2-yl) ethyl] - 1-piperazinyl} carbonyl] benzyl, 4-phenylbenzyl, 2-phenylbenzyl, 3-phenylbenzyl, 4-tert-butylbenzyl, 4-aminobenzyl, 4-nitrobenzyl, 4-methoxycarbonylbenzyl, 4-carboxybenzyl, 3-methoxy-4-chlorobenzyl, 4-methoxybenzyl, 2,4,6-trimethoxybenzyl, 3,4-dichlorobenzyl, 4-chlorobenzyl, 4-bromobenzyl, 2,4,6-trifluorobenzyl, 4-fluorobenzyl, 4-cyanobenzyl, 4-piperidinylcarbonylbenzyl, 4-anilinocarbonylbenzyl, 4- (N-cyclohexylaminocarbonyl) benzyl, 4- (N-benzoylamino) benzyl, 4- (N-cyclohexylamino) benzyl, 4-phenylcarbamoylaminobenzyl, 4-methylbenzyl, 3,4-dimethylbenzyl, 3,4,5-trimethylbenzyl, 4-benzyloxybenzyl, 4-ethylcarbamoylaminobenzyl, 4-ethylaminocarbonylbenzyl, 4-isopropylaminocarbonylbenzyl, Λ- [Ν- (2-hydroxyethyl) aminoca benzyl] benzyl, 4- [N / - (3-pyridyl) aminocarbonyl] benzyl, 4- [N / - (4-chlorophenyl) aminocarbonyl] benzyl, 4 - [/ V- (4-isopropylphenyl) aminocarbonyl] benzyl 4,4 - [[V- (4-phenoxyphenyl) aminocarbonyl] benzyl, 4- [A / - (3-phenoxyphenyl) aminocarbonyl] benzyl,

4 - [[V- (3-phenoxybenzoyl) amino] benzyl, 4- [A / - (4-phenoxybenzoyl) amino] benzyl, 4- [A / - (4-chlorobenzoyl) amino] benzyl, 4- [A / - (2-chlorobenzoyl) amino] benzyl, 4 - [[V- (2,6-dichlorobenzoyl) amino] benzyl, 4 - [[V- (4-methoxyphenyl) aminocarbonyl] benzyl, 4- [A / - (2 -furylcarbonyl) amino] benzyl, 4 - [[V- (4-methoxybenzoyl) amino] benzyl, 4- [N- (3-methoxybenzoyl) amino] benzyl, 4- [[V- (2-methoxybenzoyl) amino] benzyl,

4-phenoxybenzyl, 4-AJ-pentyloxycarbonylaminobenzyl, 4 - [[V- (4-methoxyphenoxycarbonyl) amino] benzyl, 4 - [/ V- (4-methylphenoxycarbonyl) amino] benzyl,

4-benzyloxycarbonylaminobenzyl, 4-ethanoylaminobenzyl, 4- (N-acetylamino) benzyl, 4-methylsulfonylaminobenzyl, methoxycarbonylaminobenzyl, 4- [N / - (4-isopropylphenyl) aminocarbonyl] benzyl, 4- [4- {2 - [( 1-, 2-, or 3-) imidazolyl] ethyl} -1-piperazinylcarbonyl] benzyl, 4- {4- [3-methyl- (2- '3-, or 4-) pyridyl] -1-piperazinyl carbonyl] benzyl, 4- {4- [4-methyl- (2-, 3-, or 4-) pyridyl] -1-piperazinylcarbonyl} benzyl, 4- [4- {2 - [(2-, 3-, or 4-) pyridyl] ethyl} -1-piperazinylcarbonyl] benzyl, 4- {4-4 - [(1- or 2-) naphthyl] - (1-, 2-, or 3-) piperazinylcarbonyl] benzyl, 4 - [( 1- '2-, 3-, or 4-piperazinylcarbonyl)] benzyl, 4- [2-methyl- (1-, 3-, 4-, 5-, or 6-) piperidinylcarbonyl] benzyl, 4- [3- ethoxycarbonyl- (1-, 2-, 4-, 5-, or 6-) piperidinyl] benzyl, 4- [4- (3-hydroxyphenyl) - (1-, 2-, 4-, 5-, or 6- ) piperidinyl] benzyl, 4- [4-hydroxy-4-benzyl- (1-, 2 · ， or 3-) piperidinylcarbonyl] benzyl, 4- [3-acetylamino- (1-, 2-, 4-, or 5-) pyrrolidinylcarbonyl] benzyl, 4- [A / - {2- [1-ethyl- (2- or 3-) pyrrolidinyl] ethyl} aminocar bonyl] benzyl, 4- [Λ / - {2 - [(2- or 3-) pyrrolidinyl] ethyl} aminocarbonyl] benzyl, Λ- [Ν- {2 - ([2-, 3-, or 4-] morpholine ) ethyl} aminocarbonyl] benzyl, 4- [N-

{3 - ([2- ， 3-, or 4] morpholine) propyl} aminocarbonyl] benzyl, 4- [2'6-dimethyl- (3-, 4-, or 5-) morpholinocarbonyl] benzyl, 4- [4 - (4-trifluoromethylanilino) - (1-, 2-, or 3-) piperazinylcarbonyl] benzyl, 4- {2 - [(1- '2-, 3-, or 4-) piperidinylmethyl] - (3-, 4 -, 5- or 6-) morpholinocarbonylbenzyl, 4- (N-methyl- [n-pentylaminocarbonyl) benzyl, 4- {4 - [(1- '2-, 4-, or 5-) 2' 3-Dihydro-1 H -indenyl] - (1-, 2-, or 3-) piperidinylcarbonyl] benzyl, 4- [N - (2-methylcycloexyl) aminocarbonyl] benzyl, 4-isoindolinylcarbonH-benzyl, 4- [2 -phenyl- (1-, 3-, 4- or 5-] pyrrolidinylcarbonyl] benzyl, 4- {2 - [(1-, 2-, 3-, or 4-morpholinomethyl) - (1-, 3-, 4 -, or 5-) pyrrolidinylcarbonyl] benzyl, 4- [2-dimethylaminomethyl- (1- ， 3-, 4-, or 5-] pyrrolidinylcarbonyl] benzyl, 4- {Λ / - [1- (4-fluoro - benzoyl) - (2-, 3-, or 4-) piperidinyl] - [? / - methylaminocarbonyl} benzyl, 4- [2-phenyl- (3-, 4-, or 5-) thiazolidinylcarbonyl] benzyl,

4- [[methyl] (2-methoxyanilino) carbonyl] benzyl, 4- (3-methylthioanylinocarbonyl) benzyl, 4- (2-methylthioanylinocarbonyl) benzyl,

4- (3,4-dichloroanylinocarbonyl) benzyl, 4- (4-trifluoromethoxy-4-anilinocarbonyl) benzyl, 4-anilinocarbonylbenzyl, 4- (4-chloroanylinocarbonyl) benzyl, 4- (4-methoxyanylinocarbonyl) benzyl, 4- (3 4- (2-methoxy-5-chloroanylinocarbonyl) benzyl, 4- (2-chloroanilinocarbonyl) benzyl, 4- (4-methylanylinocarbonyl) benzyl, 4- (2,4-dimethoxyanylinocarbonyl) benzyl, 4- (4-methoxy-5-chloroanylinocarbonyl) benzyl, 4- ( 2-Methoxy-5-acetylaminoanilinocarbonyl) benzyl, 4- (3,4-dimethoxyanylinocarbonyl) benzyl, 4- [2- (1-methylalyl) anylinocarbonyl] benzyl, 4- (3-trifluoromethoxyanylinocarbonyl) benzyl, 4- (2-methylanylinocarbonyl) ) benzyl, 4- (2-fluoroanilinocarbonyl) benzyl, 4- (3-fluoroanylinocarbonyl) benzyl, 4- (4-fluoroanylinocarbonyl) benzyl, 4- (3-dimethylaminoanylinocarbonyl) benzyl, 4- (4-ethoxyanylinocarbonyl) benzyl, 4- (3-Trifluoromethylanilinocarbonyl) benzyl, 4- (4-trifluoromethylanylinocarbonyl) benzyl, 4- (3-acetylaminoanylinocarbonyl) benzyl, 4- (4-acetylaminoanylinocarbonyl) benzyl, 4 - [(2-, 3-, or 4-pyridylaminoca benzyl) benzyl, 4 - [[N-methyl- (3-methylanilino) carbonyl] benzyl, 4- [3-methoxy- (2-, 4-, 5-, or 6-) pyridylaminocarbonyl] benzyl, 4- (2 - phenoxy anilinocarbonyl) benzyl,

4- (3-phenoxyanylinocarbonyl) benzyl, 4- (4-phenoxyanylinocarbonyl) benzyl, 4- (3,5-dichloroanylinocarbonyl) benzyl, 4- (2,3-dimethylanylinocarbonyl) benzyl, 4- (2,4-dimethylanylinocarbonyl) benzyl 4- (3,5-dimethylanylinocarbonyl) benzyl, 4- (3,5-difluoroanylinocarbonyl) benzyl, 4 - [(1- '2-, 3-, 4-, 5-, 6-, or 7-) indolylaminocarbonyl ] benzyl, 4- (3-fluoro-4-methoxyanylinocarbonyl) benzyl, 4- (4-aminosulfonylanylinocarbonyl) benzyl, 4- (4-methyl-3-methoxyanylinocarbonyl) benzyl, 4- (3-chloro-4-methoxyanylinocarbonyl) benzyl 4- (3-chloro-4-methylanilinocarbonyl) benzyl, 4- (3-methoxy-5-trifluoromethylanylinocarbonyl) benzyl, 4- (3-chloro-4-fluoroanylinocarbonyl) benzyl, 4- [3-methyl- (2- , 4-, 5- or 6-) pyridylaminocarbonyl] benzyl, 4 - [(2- ， 4- or 5-thiazolylaminocarbonyl) benzyl, 4- (3-chloro-4-hydroxyanylinocarbonyl) benzyl, 4- (2-chloro 5-acetylaminoanylinocarbonyl) benzyl, 4- (4-methylthioanylinocarbonyl) benzyl, 4- (4-isopropylanylinocarbonyl) benzyl, 4- (4-tert-butylanylinocarbonyl) benzyl, 4- [(2- or 4-) 1，2'-4-triazolylaminocarbonyl] benzyl, 4- {4- [2-oxo- (1-, 3-, 4-, or 5-] pyrrolidinyl] anilinocarbonyl} benzyl, 4 ( 4-methylsulfonylamino) benzyl, 4- (4-methylcarbamoylanylinocarbonyl) benzyl anilinocarbonylbenzyl, 4- (2-benzyloxyanylinocarbonyl) benzyl, 4- (4-vinylanylnocarbonyl) benzyl,

4- (4-acetylaminoanylinocarbonyl) benzyl, 4- (3-acetylaminoanylinocarbonyl) benzyl, 4- (4-trifluoromethylanylinocarbonyl) benzyl, 4- {3 - [(2-, 3-, or 4-) pyridyl] propionylamino} benzyl, 4- (3-phenoxypropionylamino) benzyl, 4 - [(2-, 3- or 4-) pyridylcarbonylamino] benzyl, 4- {2 - [(2-, 3-, or 4-) pyridyl] acetylamino} benzyl, 4 - [(2- or 3-) furylcarbonylamino] benzyl, 4 - [(2- or 3-) thienylcarbonylamino] benzyl, 4- {2 - [(2- or 3-) thienyl] acetylamino} benzyl,

4- {2 - [(1-, 2-, or 3-) pyrrolyl] - (3-, 4-, 5-, or 6-) pyridyl carbonylamide

nojbenzila,

4-cyclopentylcarbonylaminobenzyl, 4-cyclohexylcarbonylaminobenzyl, 4- (2-cyclopentylacetylamino) benzyl, 4- (2-cyclohexylcarbonylamino) benzyl,

4- [1-benzoyl- (2-, 3-, or 4-) piperidinylcarbonylamino] benzyl, 4- [1 acetyl- (2- ， 3-, or 4-) piperidinylcarbonylamino] benzyl, 4 - [(2- ， 3-, 4-, 5-, 6-, 7- or 8-) chromanyl] benzyl,

4- (2-nitrobenzoylamino) benzyl,

4- (3-nitrobenzoylamino) benzyl,

4- (4-nitrobenzoylamino) benzyl,

4- (2-phenylbenzoylamino) benzyl,

4- (2-dimethylaminobenzoylamino) benzyl,

4- (2-anilinobenzoylamino) benzyl,

4- (2,6-dichlorobenzoylamino) benzyl,

4- (2-cyanobenzoylamino) benzyl,

4- (3-phenoxybenzoylamino) benzyl,

4- (2-phenoxybenzoylamino) benzyl,

4- (4-phenoxybenzoylamino) benzyl,

4 - [(1- or 2-) naphthylcarbonylamino] benzyl,

4- (2-methyl-3-fluorobenzoylamino) benzyl,

4- (3,4-methylenedioxybenzoylamino) benzyl,

4- {2- [1，3-dioxo- (2-, 4-, or 5-) isoindolinyl] acetylamino} benzyl,

4- {2- [2-thioxo-4-oxothiazolidinyl] acetylamino} benzyl,

4- {3 - [(1-, 2-, 3-, or 4-) piperidinyl] propionylamino} benzyl,

4- (4-acetylbenzoylamino) benzyl,

4- (2-trifluoromethylbenzoylamino) benzyl,

4-

(3-Trifluoromethylbenzoylamino) benzyl, 4- (4-trifluoromethylbenzoylamino) benzyl, 4- [2- (2-chlorophenyl) acetylamino] benzyl, 4- (2-chloro-4-fluorobenzoylamino) benzyl, 4- (2-chlorocinnamoylamino) benzyl, 4- (3,4-methylenedioxycinnamoylamino) benzyl, 4- (3- (2-, 3-, or 4-) pyridylvinylcarbonylamino] benzyl, 4- [2-chloro- (3-, 4-, 5-, or 6-) pyridylcarbonylamino] benzyl, 4- {2 - [(2-, 3-, or 4-) pyridylthio] acetylamino} benzyl, 4 - [(2- ， 3-, 4-, 5-, 6-, or 7-) indolylcarbonylamino] benzyl, 4 - [(1- ， 2-, or 3-) pyrrolylcarbonylamino] benzyl, 4- [2-oxo- (1-, 3-, 4-, or 5-] pyrrolidinylcarbonylamino] benzyl , 4 - [(2- ， 3-, 4-, 5-, 6-, or 7-) benzofurylcarbonylamino] benzyl, 4- [2,6-dichloro- (3-, 4-, or 5-) pyridylcarbonylamino] benzyl,

4- {2 - [(1-, 2-, 3-, 4-, 5-, 6-, or 7-) indolyl] acetylamino} benzyl, 4 - [(2- '3-, 4-, 5- , 6-, or 7-) benzothienylcarbonylaminojbenzyl, 4- {4- [2-oxo-O-, 3-, 4-, or 5-) pyrrolidinyl] benzoylamino} benzyl, 4- {4 - [(1-, 2 -, or 3-) pyrrolyl] benzoylamino} benzyl,

4- {4 - [(1-, 3-, 4-, or 5-) pyrazolyl] benzoylamino} benzyl, 4- {4 - [(1-, 3-, or 5-) 1,2,4-triazolyl ] benzoylamino} benzyl, 4- {4 - [(1-, 2-, 4-, or 5-) imidazolyl] benzoylamino} benzyl, 4- [4- (3,5-dimethyl-4-isoxazolyl) benzoylamino] benzyl 4 - [(2- or 3-) pyrazylcarbonylamino] benzyl, 4- (2-methoxybenzoylamino) benzyl, 4- (2-methoxy-5-chlorobenzoylamino) benzyl, 4- (4-chlorobenzoylamino) benzyl, 4- (2 -phenoxyacetylamino) benzyl, 4- (3-phenylpropionyl) benzyl,

4 - [(2-, 3-, or 4-) pyridylcarbonylamino] benzyl, 4-benzoylaminobenzyl, 4-cinnamoylaminobenzyl, 4- (4-methoxyphenylsulfonylamino) benzyl, 4- (3-methoxyphenylsulfonylamino) benzyl, 4- (2-methoxyphenylsulfonylamino) ) benzyl, 5

10

15

20

25

30

4- (4-chlorophenylsulfonylamino) benzyl, 4- (3-chlorophenylsulfonylamino) benzyl, 4- (2-chlorophenylsulfonylamino) benzyl, 4- (2-methylphenylsulfonylamino) benzyl, 4- (3-methylphenylsulfonylamino) benzyl, 4- (4- methylphenylsulfonylamino) benzyl, 4- (4-fluorophenylsulfonylamino) benzyl, 4- (3-fluorophenylsulfonylamino) benzyl, 4- (2-fluorophenylsulfonylamino) benzyl, 4- (2-methoxy-5-chlorophenylsulfonylamino) benzyl, 4- (2-trifluoromethylphenyl) ) benzyl, 4- (3-trifluoromethylphenylsulfonylamino) benzyl, 4- (4-trifluoromethylphenylsulfonylamino) benzyl, 4 - [(2- or 3-) thienylsulfonylamino] benzyl, 4- (2-chlorophenylsulfonylamino) benzyl, 4- (2-trifluoromethoxyphenylsulfonyl) ) benzyl, 4- (3-trifluoromethoxyphenylsulfonylamino) benzyl, 4- (4-trifluoromethoxyphenylsulfonylamino) benzyl, 4- (2-methoxycarbonylphenylsulfonylamino) benzyl, 4- (2-cyanophenylsulfonylamino) benzyl, 4- (3-cyanophenyl) benzyl (4-cyanophenylsulfonylamino) benzyl, 4- (3,4-dimethoxyphenylsulfonylamino) benzyl, 4- (2,5-dimethoxy) phenylsulfonylamino) benzyl, 4- (2-nitrophenylsulfonylamino) benzyl, 4- (3-nitrophenylsulfonylamino) benzyl, 4- (4-nitrophenylsulfonylamino) benzyl, 4- (4-bromophenylsulfonylamino) benzyl, 4- (3-bromophenylsulfonylamino) benzyl - (2-bromophenylsulfonylamino) benzyl, 4- (4-n-butylphenylsulfonylamino) benzyl, 4- (2-methoxy-5-chlorophenylsulfonylamino) benzyl, 4- (2,6-dichlorophenylsulfonylamino) benzyl, 4 - [(1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolylsulfonylamino] benzyl, 4- [1-methyl- (2-, 4-, or 5-) imidazolylsulfonylamino] benzyl, 4- (2,3-dichlorophenylsulfonylamino) benzyl, 4- (2,5-dichlorophenylsulfonylamino) benzyl, 4- (2,4-dichlorophenylsulfonylamino) benzyl, 4- (3-nitro-4-methylphenylsulfonylamino) benzyl, 4- (2-chloro -4-fluorophenylsulfonylamino) benzyl, 4- (2,4-dichloro-5-methylphenylsulfonylamino) benzyl, 4- (2-methyl-5-nitrophenylsulfonylamino) benzyl, 4- (2-chloro-5-nitrophenylsulfonylamino) benzyl, 4- (2-chloro-4-cyanophenylsulfonylamino) benzyl, 4- (2,4,6-trimethylphenylsulfonylamino) benzyl, 4- (4-ac ethylaminophenylsulfonylamino) benzyl, 4- (3,5-dichloro-2-hydroxyphenylsulfonylamino) benzyl, 4- (4-methoxy-2-nitrophenylsulfonylamino) benzyl, 4- (3,4-dichlorophenylsulfonylamino) benzyl butylphenylsulfonylamino) benzyl, 4- (4-carboxyphenylsulfonylamino) benzyl, 4- (2-bromo-5-chlorophenylsulfonylamino) benzyl, 4- (4-ethylphenylsulfonylamino) benzyl, 4- (2,5-dimethylsulfonylamino) benzyl, 4- (4 -n-butoxyphenylsulfonylamino) benzyl, 4- (2,5-difluorophenylsulfonylamino) benzyl, 4- (2-chloro-4-acetylaminophenylsulfonylamino) benzyl, 4- (2,4-difluorophenylsulfonylamino) benzyl, 4- (2-methoxy-4) -methylphenylsulfonylamino) benzyl, 4- (2-methyl-3-chlorophenylsulfonylamino) benzyl, 4- (2,6-difluorophenylsulfonylamino) benzyl, 4- (3,4-difluorophenylsulfonylamino) benzyl, 4- (2-methyl-5-fluorophenylsulfonylamino) ) benzyl, 4- (3-methyl-4-chlorophenylsulfonylamino) benzyl, 4- (2-methyl-6-chlorophenylsulfonylamino) benzyl, 4- (4-isopropylphenylsulfonylamino) benzyl, 4- (3,4-dichlorophenylsulfonylamino) benzyl, 4 - (2-flu oro-4-bromophenylsulfonylamino) benzyl, 4- (4-methyl-3-chlorophenylsulfonylamino) benzyl, 4-vinylsulfonylaminobenzyl, 4- (3-chloropropylphenylsulfonylamino) benzyl, 4-cyclohexylmethylsulfonylaminobenzyl, 4- [2-chloro- (3- -, or 5-) thienylsulfonylamino] benzyl, 4- (3,5-dichlorophenylsulfonylamino) benzyl, 4- {4- [2- (4-methoxycarbonyl) ethyl] phenylsulfonylamino} benzyl, 4- [4-methyl- (2- , 3-, 4-, 5-, 6-, 7-, or 8-) 3,4-dihydro-2H-1'4-dihydro-2H, 4-benzoxazinylsulfonylamino] benzyl,

4- (2,2,2-trifluoroethylsulfonylamino) benzyl, 4- (2，3，5-trimethyl-4-methoxyphenylsulfonylamino) benzyl, 4 - [(1,3-dimethyl-5-chloro-4-pyrazolyl) sulfonylaminojbenzyl, 4 - [(3,5-dimethyl-4-isoxazolyl) sulfonylamino] benzyl, 4- (3-carboxy-4-hydroxyphenylsulfonylamino) benzyl, 4 - {[2,3-dichloro- (4- or 5-) thienyl] sulfonylamino} benzyl, 4 - {[2,5-dichloro- (3- or 4-) thienyl] sulfonylamino} benzyl, 4 - {[2-bromo- (3-, 4-, or 5-) thienyl] sulfonylamino} benzyl, 4- (4-carboxyphenylsulfonylamino) benzyl, 4- (2-acetylamino-4-methyl-5-thiazolylsulfonylamino) benzyl, 4 - {[2-methoxycarbonyl- (3-, 4-, or 5-) thienyl] sulfonylamino} benzyl , 4-benzylsulfonylaminobenzyl, 4-styrylsulfonylaminobenzyl, 4- (2,4,5-trifluorophenylsulfonylamino) benzyl, 4-phenylsulfonylaminobenzyl, 4-phenoxycarbonylaminobenzyl, 4 - [(4-chlorophenoxy) carbonylamino] benzyl, 4 - [(4-brom) carbonylamino] benzyl, 4-benzyloxycarbonylaminobenzyl, 4-methoxycarbonylaminobenzyl, 4-n-butoxycarbonylaminobenzyl, 4 - [(4-methoxyphenoxy) carbonylaminojbenzyl a, 4 - [(3-methoxyphenoxy) carbonylamino] benzyl, 4 - [(2-methoxyphenoxy) carbonylamino] benzyl, 4 - [(1- or 2-) naphthyloxycarbonylamino] benzyl, 4 - [(4-fluorophenoxy) carbonylamino] benzyl, 4 [(4-methylphenoxy) carbonylamino] benzyl, 4 - [(2-chlorobenzyloxy) carbonylaminojbenzyl, 4- [2-propynyloxycarbonylamino] benzyl, 4 - [(4-nitrophenoxy) carbonylaminojbenzyl, 4- (2-fluoroethoxycarbonylamino) benzyl (3-Butenyloxycarbonylamino) benzyl, 4- (4-chlorobutoxycarbonylamino) benzyl, 4- (2-chloroethoxycarbonylamino) benzyl, 4- [2- (benzyloxy) ethoxycarbonylamino] benzyl, 4-propoxycarbonylaminobenzyl, 4-n-butoxycarbonylaminobenzyl, 2-Isopropyl-5-methylcyclohexyloxycarbonylamino) benzyl, 4 - [(4-nitrobenzyloxy) carbonylamino] benzyl, 4- (2-ethylhexyloxycarbonylamino) benzyl, 4- [N-methyl- (4-chloroanilino) carbonyl] benzyl, 4- [(2-chloroanilino) carbonyl] benzyl, 4 - [(3-cyanoanilino) carbonyl] benzyl, 4 - [(4-cyanoanilino) carbonyl] benzyl, 4 - [(2-cyanoanilino) carbonyl] benzyl, 4 - [(2-chloro 4-fluoroanilino) carbonyl] benzyl , 4 - [(1- or 5-) tetrazolylaminocarbonyl] benzyl, 4- [5-methyl- (3- or 4-) isoxazolylaminocarbonyl] benzyl, 4- {4- [4-methyl- (1- ， 2-, 3-, or 4-) piperazinyl] anilinocarbonyl} benzyl, (2-, 3-, or 4-) (1-piperidinylmethyl) benzyl, (2-, 3-, or 4-) ([V-methylanylinomethyl) benzyl, (2-, 3-, or 4-) (phenylthiomethyl) benzyl, and

(2-, 3-, or 4-) (1-indolylmethyl) benzyl.

Examples of lower cycloalkylalkyl groups include C 3-8 cycloalkylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group such as cyclopropylmethyl, cyclohexylmethyl, 2-cyclopropylethyl, 1-cyclobutylethyl, cyclopentylmethyl, -cyclopentylpropyl, 4-cyclohexylbutyl, 5-cycloheptylpentyl, 6-cyclooctylhexyl, 1,1-dimethyl-2-cyclohexylethyl, and 2-methyl-3-cyclopropylpropyl.

Examples of lower alkyl phenoxy groups include phenoxy alkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as phenoxymethyl, 2-phenoxyethyl, 1-phenoxyethyl, 3-phenoxypropyl, 4-phenoxybutyl 1,1-dimethyl-2-phenoxyethyl, 5-phenoxypentyl, 6-phenoxyhexyl, 1-phenoxyisopropyl, and 2-methyl-3-phenoxypropyl.

Examples of lower alkyl naphthyl groups include naphthylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as (1- or 2-) naphthylmethyl, 2 - [(1- or 2-) naphthyl ] ethyl, 1 - [(1- or 2-) naphthyl] ethyl, 3 - [(1- or 2-) naphthyl] propyl, 4 - [(1- or 2-) naphthyl] butyl, 5- [ (1- or 2-) naphthyl] pentyl, 6 - [(1- or 2-) naphthyl] hexyl, 1,1-dimethyl-2 - [(1- or 2-) naphthyl] ethyl, and 2- methyl-3 - [(1- or 2-) naphthyl] propyl. Examples of lower alkyl alkoxy groups include alkoxy groups.

wherein the alkyl moiety is a straight or branched C1-6 alkyl group and the alkoxy moiety is a straight or branched C1-6 alkoxy group such as methoxymethyl, 2-methoxyethyl, 1-ethoxyethyl, 2 -ethoxyethyl, 3-n-butoxypropyl, 4'-propoxybutyl, 1-methyl-3-isobutoxypropyl, 1,1-dimethyl-2-n-pentyloxyethyl, 5-n-hexyloxypentyl, 6-methoxyhexyl, 1-ethoxyisopropyl, and 2-methyl-3-methoxypropyl.

Examples of lower alkyl carboxy groups include carboxyalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as carboxymethyl, 2-carboxyethyl, 1-carboxyethyl, 3-carboxypropyl, 4- carboxybutyl, 5-carboxypentyl, 6-carboxyhexyl, 1,1-dimethyl-2-carboxyethyl, and 2-methyl-3-carboxypropyl.

Examples of lower alkyl lower alkoxycarboxyl groups include

in alkoxycarbonylalkyl groups wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group and the alkyl moiety is a straight or branched C1-6 alkyl group such as methoxycarbonylmethyl, ethoxycarbonylmethyl, 2-methoxycarbonylethyl, 2 -ethoxycarbonylethyl, 1-ethoxycarbonylethyl, 3-methoxycarbonylpropyl, 3-ethoxycarbonylpropyl, 4-ethoxycarbonylbutyl, 5-isopropoxycarbonylpentyl, 1,1-dimethyl-2-n-butoxycarbonyl-2-methyl-3-merceryl butoxycarbonylpropyl, 2-n-pentyloxycarbonylethyl, and n-hexyloxycarbonyl methyl.

Examples of piperazine ring optionally substituted piperazinyl groups with one or more members selected from the group consisting of a phenyl group and lower alkyl groups include: piperazine ring optionally substituted piperazinyl groups

one with one to three members selected from the group consisting of a phenyl group and straight and branched C1-6 alkyl groups;

such as (1- or 2-) piperazinyl, 4-methyl- (1-, 2-, or 3-) piperazinyl, 4-ethyl- (1-, 2-, or 3-) piperazinyl, 4-n -propyl-1-, 2-, or 3-) piperazinyl, A-tert-butyl- (1- '2-, or 3-) piperazinyl, 4-sec-butyl- (1-, 2-, or 3- ) piperazinyl, 4- n -butyl- (1-, 2-, or 3-) piperazinyl, 4-n-pentyl- (1-, 2-, or 3-) piperazinyl, 4-n-hexyl- (1- , 2-, or 3-) piperazinyl, 3,4-dimethyl- (1-, 2-, 5-, or 6-) piperazinyl, 3，4，5-trimethyl- (1- or 2-) piperazinyl, 4 -phenyl- (1- '2-, or 3-) piperazinyl, 2,4-diphenyl- (1-, 3-, 5-, or 6-) piperazinyl, 2,3,4-triphenyl- (1-' 5-, or 6-) piperazinyl, and 4-phenyl-2-methyl- (1-, 3-, 5-, or 6-) piperazinyl.

Examples of pyridylamino groups include (2- ， 3-, or 4-) pyridylamino.

Examples of pyridylcarbonylamino groups include (2-, 3-, or 4-) pyridylcarbonylamino.

Examples of anilino groups optionally substituted on the amino group with one or more lower alkyl groups include optionally substituted anilino groups on the amino group with one or more linear and / or branched C1-6 alkyl groups, such as anilino, Î ± -methylanilino, N-ethylanilino, N-propylanilino, N-isopropylanilino, N-butylanilino, N-sec-butylanilino, N-tert-butylanilino, N-pentylanilino and N-hexylanilino. Examples of optionally substituted lower alkyl pyridyl groups

in the pyridine ring with one or more members selected from the group

consisting of halogen atoms; piperidinyl groups; a morphfoH-group; piperazinyl groups optionally substituted on the piperizine ring with one or more members selected from the group consisting of a phenyl group and lower alkyl groups; thienyl groups; a phenyl group; pyridyl groups; piperidinyl lower alkyl groups; phenyl lower alkyl groups; biphenyl groups;

lower alkyl groups optionally substituted with one or more halogen atoms; pyridylamino groups; pyridylcarbonylamino groups; lower alkoxy groups; lower alkyl anilyl groups optionally substituted on the amino group with one or more lower alkyl groups; and anilino groups optionally substituted on the amino group with one or more lower alkyl groups include: alkyl pyridyl groups wherein the alkyl moiety is an alkyl group.

straight or branched C1-6 kyl, optionally substituted on the one to three membered pyridine ring selected from the group consisting of the halogen atoms described above; piperidinyl groups; a morpholino group; the above-described piperazinyl groups optionally substituted on the one- to three-membered piperazine ring selected from the group consisting of a phenyl group and straight and branched C1-6 alkyl groups; thienyl groups; a phenyl group; pyridyl groups; piperidinylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group; phenylthioalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group; biphenyl groups; lower alkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted with one to three halogen atoms; pyridylamino groups; pyridylcarbonylamino groups; straight and branched C1-6 alkoxy groups; anilinoalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the amino group with one or two straight and / or branched C 1-6 alkyl groups; and the above described anilino groups optionally substituted on the amino group by one or more straight and / or branched C1-6 alkyl groups;

such as (2-, 3-, or 4-) pyridylmethyl, 2 - [(2-, 3-, or 4-) pyridyl] ethyl, 1 - [(2-, 3-, or 4-) pyridyl] ethyl , 3 - [(2-, 3-, or 4-) pyridyl] propyl, 4 - [(2-, 3-, or 4-) pyridyl] butyl, 1,1-dimethyl-2 - [(2-, 3-, or 4-) pyridyl] ethyl, 5 - [(2-, 3-, or 4-) pyridyl] pentyl, 6 - [(2-, 3-, or 4-) pyridyl] hexyl, 1 - [(2-, 3-, or 4-) pyridyl] isopropyl, 2-methyl-3 - [(2-, 3-, or 4-) pyridyl] propyl, (2-chloro-3-pyridyl) methyl, [2-chloro- (3-, 4-, 5-, or 6-) pyridyl] methyl, [2,3-dichloro- (4-, 5-, or 6-) pyridyl] methyl, [2-bromo] (3-

4-, 5-, or 6-) pyridyl] methyl, [2,4,6-trifluoro- (3-, 5-, or 6-) pyridyl] methyl, [2- (1-piperidinyl) - (3- , 4-, 5-, or 6-) pyridyl] methyl, [2- (4-morpholino) - (3-, 4-, 5-, or 6-) pyridyl] methyl, [2- (4-methylphenyl) 1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] methyl, 2- [2- (4-

ethyl-1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] ethyl, 3- [2- (4-isopropyl-1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] propyl, 4- [2- (4-sec-butyl-1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] butyl, 5- [2- (4 -n-pentyl-1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] pentyl, 6- [2- (4-n-hexyl-1-piperazinyl) - (3-, 4 -, 5-, or 6-) pyridyl] hexyl, [2- (4-phenyl-2-methyl-1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] methyl, [2 - (4-phenyl-1-piperazinyl) - (3-, 4-, 5-, or 6-) pyridyl] methyl, [2- (3-thienyl) - (3-, 4-, 5-, or 6 -) pyridyl] methyl, [2-phenyl- (3-, 4-,

5-, or 6-) pyridyl] methyl, 2- [2,4-diphenyl- (3-, 5-, or 6-) pyridyl] ethyl, 3- [2- (2-pyridyl) -

6- (3-thienyl) - (3-, 4-, or 5-) pyridyl] propyl, 4- (3-anilino- (2-, 4-, 5-, or 6-) pyridylbutyl, 5- [2- (4-morpholino) - (3-, 4-, 5-, or 6-) pyridyl] pentyl, 6- [2- (1-piperidinyl) - (3-, 4-, 5-, or 6 -) pyridyl] hexyl, [2- (2-pyridyl) - (3-, 4-, 5-, or 6-) pyridyl] methyl, (3-, 4-,

5-, or 6-) (1-piperidinylmethyl) -2-pyridylmethyl, (3-, 4-, 5-, or 6-) phenylthiomethyl-2-pyridylmethyl, (4-, 5-, or 6-) biphenyl- (4-, 5-, or 6-) trifluoromethyl-3-pyridylmethyl, (4-, 5-, or 6-) (2-pyridylamino) -3-pyridylmethyl, (4-, 5-, or 6-) [(2- or 3-) pyridylcarbonylamino] -3-pyridylmethyl, 3,5-dimethyl-4-methoxy-2-pyridylmethyl, (3-, 4-, 5-, or 6-) (A / - methylanilinomethyl) -2-pyridylmethyl, [2- (N-methylanilino) - (3-, 4-, 5-, or 6-) pyridyl] methyl, 2- [2- (N-ethylanilino) - (3- , 4-, 5-, or 6-) pyridyl] ethyl, 3- [2- (V-propylanilino) - (3-, 4-, 5-, or 6-) pyridyl] propyl, 4- [ 2 - ([Î ± -butylanilino) - (3-, 4-, 5-, or 6-) pyridyl] ethyl, 5- [2- (β-pentylanilino) - (3-, 4-, 5-, or 6-) pyridyl] pentyl, and 6- [2- (N-β-hexylanilino) - (3-, 4-, 5-, or 6-) pyridyl] hexyl.

Examples of cyano lower alkyl groups include cyanoalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, such as cyanomethyl, 2-cyanoethyl, 1-cyanoethyl, 3-cyanopropyl, 4-cyano- butyl, 1,1-dimethyl-2-cyanoethyl, 5-cyanopentyl, 6-cyanohexyl, 1-cyanoisopropyl, and 2-methyl-3-cyanopropyl.

Examples of quinolyl lower alkyl groups include quinolylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, such as [(2-, 3-, 4-, 5-, 6-, 7 -, or 8-) quinolyl] methyl, 2 - [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolyl] ethyl, 1 - [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolyl] ethyl, 3 - [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolyl] propyl, 4 - [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolinyl] butyl, 1,1-dimethyl-2 - [(2-, 3-, 4- , 5-, 6-, 7-, or 8-) quinolyl] ethyl, 5 - [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolyl] pentyl, 6- [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolyl] hexyl, 1 - [(2-, 3-, 4-, 5-, 6-, 7-, or 8-) quinolyl] isopropyl, and 2-methyl-3 - [(2-, 3-, 4-, 5-, 6-, 7-, or -8) quinolylpropyl.

Examples of lower alkoxy substituted lower alkyl groups lower alkoxy include alkoxyalkoxy substituted alkyl groups wherein each of the two alkoxy moieties is a straight or branched C1-6 alkoxy group and the alkyl moiety is a linear C1-6 alkyl group or branched, such as methoxymethoxymethyl, 2- (methoxymethoxy) ethyl, 1- (ethoxymethoxy) ethyl, 3- (2'-β-buoxyethoxy) propyl, 4- (3-n-propoxypropoxy) butyl, 1,1- dimethyl-2- (4-n-pentyloxybutoxy) ethyl, 5- (5-n-hexyloxypentyloxy) pentyl, 6- (6-methoxyhexyloxy) hexyl, 1-ethoxymethoxyisopropyl, 2-methyl-3- (2-methoxyethoxy) propyl, and 3,3-dimethyl-3- (methoxymethoxy) propyl. Examples of hydroxy-substituted lower alkyl groups include

include straight and branched C1-6 alkyl groups substituted with one to three hydroxy groups such as hydroxymethyl, 2-hydroxyethyl, 1-hydroxyethyl, 3-hydroxypropyl, 2,3-dihydroxypropyl, 4-hydroxybutyl, 3,4-dihydroxybutyl, 1 , 1-Dimethyl-2-hydroxyethyl, 5-hydroxypentyl, 6-hydroxyhexyl, 3,3-dimethyl-3-hydroxypropyl, 2-methyl-3-hydroxypropyl, and 2,3,4-trihydroxybutyl.

Examples of lower thiazolyl alkyl groups optionally substituted on the triazole ring with one or more members selected from the group consisting of halogen atoms, a phenyl group, thienyl groups, and pyridyl groups include:

thiazolylalkyl groups wherein the alkyl moiety is a C1-6 group

straight or branched alkyl, optionally substituted on the triazole ring with one to three members selected from the group consisting of halogen atoms, a phenyl group, thienyl groups, and pyridyl groups;

such as [(2-, 4-, or 5-) thiazolyl] methyl, 2 - [(2-, 4-, or 5-) thiazo-1-methyl] 1 - [(2-, 4-, or 5-) thiazolyl ] ethyl, 3 - [(2-, 4-, or 5-) thiazolyl] propyl, 4 - [(2-, 4-, or 5-) thiazolyl] butyl, 5 - [(2-, 4-, or 5- ) thiazolylpentyl, 6 - [(2-, 4-, or 5-) thiazoylhexyl 1,1-dimethyl-2 - [(2-, 4-, or 5-) thiazolyljetyl, [2-methyl-3- [ (2-, 4-, or 5-) thiazolyl] propyl, [2-chloro- (4- or 5-) thiazolyl] methyl, 2- [2-chloro- (4- or 5-) thiazolyl] ethyl 1- [2-fluoro- (4- or 5-) thiazolyl] ethyl, 3- [2-bromo- (4- or 5-) thiazolyl] propyl, 4- [2-iodo- (4- or 5- ) thiazolyl] butyl, [2-phenyl- (4- or 5-) thiazolyl] methyl, 2- [2-phenyl- (4- or 5-) thiazolyl] ethyl, 1- [2-phenyl- (4- or 5-) thiazolyl] ethyl, 3- [2-phenyl- (4- or 5-) thiazolyl] propyl, 4- [2-phenyl- (4- or 5-) thiazolyl] butyl 5- [2- phenyl- (4- or 5-) thiazolyl] pentyl, 6- [2-phenyl- (4- or 5-) thiazolyl] hexyl, 1,1-dimethyl-2- [2-phenyl- (4- or 5-) thiazolyl ] ethyl, [2-methyl-3- [2-phenyl- (4- or 5-) thiazolyl] propyl, [2- (2- or 3-) thienyl- (4- or 5-) thiazolyl] methyl , 2- [2- (2- or 3-) thienyl - (4- or 5-) thiazolyl] ethyl, 1- [2- (2- or 3-) thienyl- (4- or 5-) thiazolyl] ethyl, 3- [2- (2- or 3-) thienyl - (4- or 5-) thiazolyl] propyl, 4- [2- (2- or 3-) thienyl- (4- or 5-) thiazolyl] butyl, 5- [2- (2- or 3-) thienyl - (4- or 5-) thiazolyl] pentyl, 6- [2- (2- or 3-) thienyl- (4- or 5-) thiazolyl] hexyl, 1,1-dimethyl-2- [2- (2 - or 3-) thienyl- (4- or 5-) thiazolyl] ethyl, [2-methyl-3- [2- (2- or 3-) thienyl- (4- or 5-) thiazolyl] propyl, [2 - (2-, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] methyl, 2- [2- (2-, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] ethyl, 1- [2- (2-, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] ethyl, 3- [2- (2-, 3-, or 4-) pyridyl - (4- or 5-) thiazolyl] propyl, 4- [2- (2-, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] butyl, 5- [2- (2 -, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] pentyl, 6- [2- (2-, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] hexyl 1,1-dimethyl-2- [2- (2-, 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] ethyl, and [2-methyl-3- [2- (2- , 3-, or 4-) pyridyl- (4- or 5-) thiazolyl] propyl.

Examples of lower alkylsilyloxy alkyl groups include alkylsilyloxyalkyl groups wherein each of the two alkyl moieties is a straight or branched C1-6 alkyl group, such as trimethylsilyloxymethyl, (1- or 2-) (triethylsilyloxy) ethyl, 3- (trimethylsilyloxy) ) propyl, dimethyl-tert-butylsilyloxymethyl, 2- (dimethyl-tert-butylsilyloxy) ethyl, 3- (dimethyl-tert-butylsilyloxy) propyl, 4- (dimethyl-tert-butylsilyloxy) butyl, 5- (dimethyl-tertyl) -butylsilyloxy) pentyl, and 6- (dimethyl-tert-butylsilyloxy) hexyl.

Examples of optionally substituted lower alkyl phenoxy groups on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups; halogen atoms; lower alkenyl groups, cycloalkyl groups, a nitro group; and a phenyl group include:

alkyl phenoxy groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the one- to three-membered phenyl ring selected from the group consisting of straight and branched C1-6 alkyl groups optionally substituted with one to three atoms halogen; straight and branched C1-6 alkoxy groups; halogen atoms;

straight and branched C 2-6 alkenyl groups; C 3-8 cycloalkyl groups; a nitro group; and a phenyl group;

such as 3 - [(2-, 3-, or 4-) methylphenoxy] propyl, 3 - [(2-, 3-, or 4-) propylphenoxy] propyl, 3 - [(2-, 3-, or 4 -) methoxyphenoxy] propyl, 3 - [(2, 3- or 3,4-dichlorophenoxy] propyl, 3 - [(2, 3- or 3,4) difluorophenoxy] propyl, 3- [3-fluoro-4-chlorophenoxy ] propyl, 3 - [(2-, 3-, or 4-) trifluoromethylphenoxy] propyl, 3- [2-methoxy-4-propenylphenoxy] propyl, 3- [2-chloro-4-methoxyphenoxy] propyl, (2- , 3-, or 4-) cyclopentylphenoxypropyl, 3 - [(2-, 3-, or 4-) nitrophenoxy] propyl, 3 - [(2, 3- or 3,4) dimethylphenoxy] propyl, and 3 - [(2-, 3-, or 4-) phenylphenoxy] propyl.

Examples of optionally substituted phenyl lower alkyl phenyl groups on the phenyl ring having one or more halogen atoms include:

phenylthioalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the phenyl ring with one to three halogen atoms;

such as phenylthiomethyl, 2-phenylthioethyl, 1-phenylthioethyl, 3-phenylthiopropyl, 4-phenylthiobutyl, 5-phenylthiopentyl, 6-phenylthiohexyl, 1,1-dimethyl-2-phenylthioethyl, 2-methyl-3-phenylthiopropyl, (2-, 3-, or 4-) chlorophenylthiomethyl, 2 - [(2-, 3-, or 4-) chlorophenylthio] ethyl, 3 - [(2-, 3-, or 4-) chlorophenylthio] propyl, 4 - [(2-, 3-, or 4-) fluoro-phenylthio] butyl, 5 - [(2-, 3-, or 4-) bromophenylthio] pentyl, and 6 - [(2-, 3-, or 4 -) iodo-phenylthio] hexyl.

Examples of optionally lower alkyl piperidinyl groups

piperidine ring substituted with one or more members selected from the group consisting of a phenyl group and lower alkyl phenyl groups include:

Piperidinylalkyl groups wherein the alkyl moiety is a branched or branched C 1-6 alkyl group, optionally substituted on the piperidine ring with one to three members selected from the group consisting of a phenyl group and phenylalkyl groups wherein the alkyl moiety is a C 1-6 alkyl group. 6 straight or branched alkyl; such as [(1-, 2-, 3-, or 4-) piperidinyl] methyl, 2 - [(1-, 2-, 3-, or 4-) piperidinyl] ethyl, 1 - [(1-, 2 -, 3-, or 4-) piperidinyl] ethyl, 3 - [(1-, 2-, 3-, or 4-) piperidinyl] propyl, 4 - [(1-, 2-, 3-, or 4-) piperidinyl] butyl, 5 - [(1-, 2-, 3-, or 4-) piperidinyl] pentyl, 6 - [(1-, 2-, 3-, or 4-) piperidinyl] hexyl, 1 , 1-dimethyl-2 - [(1-, 2-, 3-, or 4-) piperidinyl] ethyl, 2-methyl-3 - [(1-, 2-, 3-, or 4-) piperidinyl] propyl , [4-phenyl-1-piperidinyl] methyl, 3- [4-phenyl-1-piperidinyl] propyl, [4-phenylmethyl-1-piperidinyl] methyl, 3- [4-phenylmethyl-1-piperidinyl] propyl , 2- [4-phenyl- (1-, 2-, or 3-) piperidinyl] ethyl, 3- [4-phenylmethyl- (1-, 2-, or 3-) piperidinyl] propyl, 4- [4- phenylethyl- (1-, 2-, or 3-) piperidinyl] butyl, 5- [4-phenyl- (1-, 2-, or 3-) piperidinyl] pentyl, and 6- [4-phenyl- ( 1-, 2-, or 3-) piperidinyl] hexyl.

Examples of lower alkyl piperazinyl groups optionally substituted on the piperazine ring with one or more phenyl groups include:

piperazinylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the piperazine ring with one to three phenyl groups;

such as (1- or 2-) piperazinylmethyl, 2 - [(1- or 2-) piperazinyl] ethyl, [4-phenyl- (1-, 2-, or 3-) piperazinylmethyl, 2- [4- phenyl- (1-, 2-, or 3-) piperazinyl] ethyl, 3- [4-phenyl- (1-, 2-, or 3-) piperazinyl] propyl, 4- [4-phenyl- (1 -, 2-, or 3-) piperazinyl] butyl, 5- [4-phenyl- (1-, 2-, or 3-) piperazinyl] pentyl, and 6- [4-phenyl- (1-, 2-, or 3-) piperazinyl] hexyl.

Examples of 1,2,3,4-tetrahydroisoquinolyl lower alkyl groups include 1,2,3,4-tetrahydroisoquinolylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group such as (1,2,3 , 4-Tetrahydroisoquinolin-2-yl) methyl, 2- (1,2,3,4-tetrahydroisoquinolin-2-yl) ethyl, 3- (1,2,3,4-tetrahydroisoquinolin-2-yl) propyl , 4- (1,2,3,4-tetrahydroisoquinolin-2-yl) butyl, 5- (1,2,3,4-tetrahydroisoquinolin-2-yl) pentyl, and 6- (1,2,3,4 -tetrahydroisoquinolin-

2-yl) hexyl.

Examples of lower alkyl naphthyloxy groups include naphthyloxyalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as 1-naphthyloxymethyl, 2- (2-naphthyloxy) ethyl, 3- (1- naphthyloxy) propyl,

3- (2-naphthyloxy) propyl, 4- (1-naphthyloxy) butyl, 5- (2-naphthyloxy) pentyl and 6- (1-naphthyloxy) hexyl. Examples of benzothiazolyloxy lower alkyl group optionally substituted on the benzothiazole ring with one or more alkyl groups include:

benzothiazolyloxyalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the benzothiazoline ring with one to three straight and / or branched C1-6 alkyl groups;

such as 1- [benzothiazol- (2-, 4-, 5-, 6-or 7-) yloxy] methyl, 2- [benzothiazol- (2-, 4-, 5-, 6-or 7-) yloxy] ethyl, 3- [benzothiazol- (2-, 4-, 5-, 6-or 7-) yloxy] propyl, 3- [benzothiazol- (2-, 4-, 5-, 6-or 7 -) yloxy] propyl, 4- [benzothiazol- (2-, 4-, 5-, 6-or 7-) yloxy] butyl, 5- [benzothiazol- (2-, 4-, 5-, 6-or 7 -) yloxy] pentyl, 6- [benzothiazol- (2-, 4-, 5-, 6-or 7-) yloxyhexyl, 2-methylbenzothiazol-5-yloxymethyl, 2- (2-methylbenzothiazol-5-yloxy) ethyl, 3- (2-methylbenzothiazol-5-yloxy) propyl, 4- (2-ethylbenzothiazol-5-yloxy) butyl, 5- (2-ethylbenzothiazol-5-yloxy) pentyl, and 6- (2-ethylbenzothiazol-5-yloxy ) hexyl.

Examples of lower alkyl groups substituted with one or more members selected from the group consisting of quinolyloxy groups and quinolyloxy isogroups include:

alkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group substituted with one to three members selected from the group consisting of quinolyloxy groups and isoquinolyloxy groups; such as (5-quinolyloxy) methyl, 2- (5-quinolyloxy) ethyl, 3- (5-quinoline)

nolyloxy) propyl, 4- (5-quinolyloxy) butyl, 5- (5-quinolyloxy) pentyl, 6- (5-quinolyloxy) hexyl, (5-isoquinolyloxy) methyl, 2- (5-isoquinolyloxy) ethyl, 3 - (5-isoquinoloxy) propyl, 4- (5-isoquinolyloxy) butyl, 5- (5-isoquinolyloxy) pentyl, and 6- (5-isoquinolyloxy) hexyl.

Examples of pyridyloxy lower alkyl groups optionally

substituted on the pyridine ring with one or more lower alkyl groups include: pyridyloxyalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the pyridine ring with one to three C 1-6 alkyl groups linear and / or branched; such as (2-, 3-, or 4-) pyridyloxymethyl, 2 - [(2-, 3-, or 4-) pyridyloxy]

ethyl, 1 - [(2-, 3-, or 4-) pyridyloxy] ethyl, 3 - [(2-, 3-, or 4-) pyridyloxy] propyl, 4 - [(2-, 3-, or 4 -) pyridyloxy] butyl, 1,1-dimethyl-2 - [(2-, 3-, or 4-) pyridyloxy] ethyl, 5 - [(2-, 3-, or 4-) pyridyloxy] pentyl, 6- [(2-, 3-, or 4-) pyridyloxy] hexyl, [6-methyl- (2-, 3-, 4-, or 5-) pyridyloxy] methyl, 2- [6-ethyl- (2-, 3-, 4-, or 5-) pyridyloxy] ethyl, 3- [6-methyl- (2-, 3-, 4-, or 5-) pyridyloxy] propyl, 4- [6-methyl- (2-, 3-, 4-, or 5-) pyridyloxy] butyl, 5- [6-methyl- (2-, 3-, 4-, or 5-) pyridyloxy] pentyl, and 6- [6-methyl- (2- , 3-, 4-, or 5-) pyridyloxy] hexyl.

Examples of lower alkoxy carboxy groups include carboxyalkoxy groups wherein the alkoxy moiety is a branched or straight C1-6 alkoxy group, such as carboxymethoxy, 2-carboxyoxy, 1-carboxyoxy, 3-carboxypropoxy, 4-carboxyoxy, 5-carboxypentyloxy, 6-carboxyhexyloxy, 1,1-dimethyl-2-carboxyoxy, and 2-methyl-3-carboxypropoxy.

Examples of lower alkoxy lower alkoxycarbonyl groups include alkoxycarbonylalkoxy groups wherein each of the two alkoxy moieties is a branched or straight C1-6 alkoxy group, such as methoxycarbonylmethoxy, ethoxycarbonylmethoxy, 2-methoxycarbonyloxyoxy, 1-ethoxycarbonyloxyoxyethyloxy , 3-Methoxycarbonylpropoxy, 3-ethoxycarbonylpropoxy, 4-ethoxycarbonylbutoxy, 5-isopropoxycarbonylpentyloxy, 6-n-propoxycarbonylhexyloxy, 1,1-dimethyl-2-n-butoxycarbonyloxy, 2-methyl-3-tert-butoxycarbonylpropoxy pentyloxycarbonyloxy, and R-hexyloxycarbonylmethoxy.

Examples of lower alkyl groups optionally substituted with one or more halogen atoms include straight and branched C1-6 alkyl groups optionally substituted with one to three halogen atoms, such as, in addition to lower alkyl, trifluoromethyl, trichloromethyl, chloromethyl, bromomethyl, fluoromethyl, iodomethyl, difluoromethyl, dibromomethyl,

2-chloroethyl, 2,2,2-trifluoroethyl, 2,2,2-trichloroethyl, 3-chloropropyl, 2,3-dichloropropyl, 4,4,4-trichlorobutyl, 4-fluorobutyl, 4,4,4-t trifluorobutyl, 5-chloropentyl,

3-Chloro-2-methylpropyl, 5-bromohexyl, and 5,6-dibromhexyl described above.

Examples of optionally substituted lower alkylthio groups

with one or more halogen atoms include straight and branched C1-6 alkylthio groups optionally substituted with one to three halogen atoms such as, in addition to the lower alkylthio, trifluoromethylthio, trichloromethylthio, chloromethylthio, fluoromethylthio, iodomethylthio, difluoromethylthio, - bromomethylthio, 2-chloroethylthio, 2,2,2-trifluoroethylthio, 2,2,2-trichloroethylthio, 3-chloropropylthio, 2,3-dichloropropylthio, 4,4,4-trichlorobutylthio, 4-fluorobutylthio, 4,4 4-Trifluorobutylthio, 5-chloropentylthio, 3-chloro-2-methylpropylthio, 5-bromohexylthio, and 5,6-dibromohexylthio described above.

Examples of lower alkylsulfonyl groups include straight and branched C1-6 alkylsulfonyl groups optionally substituted with one to three halogen atoms, such as methylsulfonyl, ethylsulfonyl, n-propylsulfonyl, isopropylsulfonyl, n-butylsulfonyl, isobutylsulfonyl, tert-butylsulfonyl , sec-butylsulfonyl, n-pentylsulfonyl, isopentylsulfonyl, neopentylsulfonyl, n-hexylsulfonyl, isoexylsulfonyl, and 3-methylpentylsulfonyl.

Examples of phenyl lower alkyl groups include phenylalkenyl groups containing one to three double bonds wherein the alkenyl moiety is a straight or branched C2- and alkenyl group, such as styryl, 3-phenyl-2-propenyl (trivial name: cinamyl ), 4-phenyl-2-butenyl, 4-phenyl-3-butenyl, 5-phenyl-4-pentenyl, 5-phenyl-3-pentenyl, 6-phenyl-5-hexenyl, 6-phenyl-4-hexenyl, 6-phenyl-3-hexenyl, 4-phenyl-1,3-butadienyl, and 6-phenyl-1,3,5-hexatrienyl.

Examples of lower alkanoyloxy groups include straight and branched C 2-6 alkanoyl groups such as acetyloxy, propionyloxy, butyryloxy, isobutyryloxy, pentanoyloxy, tert-butylcarbonyloxy, and hexanoyloxy.

Examples of phenyl lower alkoxy groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; lower alkylthio groups optionally substituted with one or more halogen atoms; lower alkoxy groups; a nitro group; lower alkylsulfonyl groups; lower alkoxycarbonyl groups; phenyl lower alkyl groups; lower alkanoyloxy groups; and 1,2,3-thiadiazolyl groups include:

phenylalkoxy groups wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group, optionally substituted on the phenyl ring with one to three members selected from the group consisting of the halogen atoms described above; the linear and branched C1-6 alkyl groups described above optionally substituted with one to three halogen atoms; the linear and branched C1-6 alkylthio groups described above optionally substituted with one to three halogen atoms; the linear and branched C1-6 alkoxy groups described above; a nitro group; the branched and branched C1-6 alkylsulfonyl groups described above; the linear and branched C1-6 alkoxycarbonyl groups described above; the phenylalkenyl groups described above having one to three double bonds wherein the alkenyl moiety is a straight or branched C 2-6 alkenyl group; the linear and branched C1-6 alkanoyloxy groups described above; and 1,2,3-thiadiazolyl groups;

such as benzyloxy, 2-phenylethyloxy, 1-phenylethyloxy, 3-phenylpropoxy, 4-phenylbutoxy, 5-phenylpentyloxy, 6-phenylexyloxy, 1,1-dimethyl-2-phenylethyloxy, 2-methyl-3-phenylpropoxy, 4-chlorobenzyloxy, 2-chlorobenzyloxy, 3-chlorobenzyloxy, 3-fluorobenzyloxy, 4-fluorobenzyloxy, 2,4-dibromobenzyloxy, 2,4,6-trifluorobenzyloxy, 3-trifluoromethylbenzyloxy, 4-trifluoromethylbenzyloxy, 4-methylbenzyloxy, 3-methyloxy 2,4-dimethylbenzyloxy, 2,4,6-trimethylbenzyloxy, 4-methoxycarbonylbenzyloxy, 3-methoxybenzyloxy, 2-methoxybenzyloxy, 3-methoxycarbonylbenzyloxy, 2,3-dimethoxybenzyloxy, 2,4,5-trimethoxybenzyloxy, 3 2- (2,3-dinitrophenyl) ethoxy, 3- (2,4,6-trinitrophenyl) ethoxy, 2-nitro-4-methylbenzyloxy, 4-methylsulfonylbenzyloxy, 4- (4-ethylsulfonylphenyl) butoxy, 5- (4- propylsulfonylphenyl) pentyloxy, 4-acetyloxybenzyloxy, 6- (4-propionyloxyphenyl) hexyloxy, 4-styrylbenzyloxy, 4- (1,2,3-thiadiazol-4-yl) benzyloxy, 4-trifluoromethylthiobenzyloxy, 3-methylthiobenzyloxy 2,4-dimethylthiobenzyloxy; and 2,4,6-trimethylthiobenzyloxy.

Examples of lower alkoxypiperidinyl groups optionally substituted on the piperidine ring with one or more lower alkyl groups include:

piperidinylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group, optionally substituted on the piperidine ring with one to three straight and / or branched C1-6 alkyl groups;

such as [(1-, 2-, 3-, or 4-) piperidinyl] methoxy, 2 - [(1-, 2-, 3-, or 4-) piperidinyl] ethoxy, 1 - [(1-, 2 -, 3-, or 4-) piperidinyl] ethoxy, 3 - [(1-, 2-, 3-, or 4-) piperidinyl] propoxy, 4 - [(1-, 2-, 3-, or 4-) piperidinyl] butoxy, 5 - [(1-, 2-, 3-, or 4-) piperidinyl] pentyloxy, 6 - [(1-, 2-, 3-, or 4-) piperidinyl] hexyloxy, 1 , 1-dimethyl-2 - [(1-, 2-, 3-, or 4-) piperidinyl] ethoxy, 2-methyl-3 - [(1-, 2-, 3-, or 4-) piperidinyl] propoxy , [1-methyl- (2-, 3-, or 4-) piperidinyl] methoxy, 2- [1-ethyl- (2-, 3-, or 4-) piperidinyl] ethoxy, 3- [1-n- propyl- (2-, 3-, or 4-) piperidinyl] propoxy, 4- [1-n-butyl- (2-, 3-, or 4-piperidinyl) butoxy, 5- [1-n-pentyl- ( 2-, 3-, or 4-) piperidinyl] pentyloxy, 6- [1-n-hexyl- (2-, 3-, or

4-) piperidinyl] hexyloxy, [1,2-dimethyl- (3-, 4-, 5-, or 6-) piperidinyl] methoxy, [1,2,3-trimethyl- (4-, 5-, or 6 -) piperidinyl] methoxy, 2- [2-n-propyl- (3-, 4-, 5-, or 6-) piperi-

dinyl] ethoxy, 2- [3-ethyl- (2-, 4-, 5-, or 6-) piperidinyljetoxy, and [2-methyl-4-isopropyl- (3-,

5-, or 6-piperidinyl) methoxy.

Examples of optionally substituted lower amino-substituted alkoxy groups in each amino group with one or more lower alkyl-branched C1-6 alkoxy groups optionally substituted amino-substituted C1-6 amino groups with one or two linear C1-6 alkyl groups and / or branched, such as aminomethoxy, 2-amino-methoxy, 1-aminoethoxy, 3-aminopropoxy, 4-aminobutoxy, 5-aminopentyloxy, 6-aminoexyloxy, 1,1-dimethyl-2-aminoethoxy, 2-methyl-3 -aminopropoxy, methylamino-methoxy, 1-ethylaminoethoxy, 2-n-propylaminoethoxy, 3-isopropylaminopropoxy, 4-7-butylaminobutoxy, 5-n-pentylaminopentyloxy, 6-n-hexylaminoexyloxy, dimethylaminoethyl-2-dimethylamino, diisopropylaminoethoxy, (V-ethyl- [N-propylamino) methoxy, and 2- (N-methyl- [N-hexylamino) ethoxy.

Examples of lower alkenyloxy groups include straight and branched C 2-6 chenyloxy groups containing one to three double bonds, such as vinyloxy, 1-propenyloxy, 1-methyl-1-propenyloxy, 2-methyl-1-propenyloxy, 2-pro - penyloxy, 2-butenyloxy, 1-butenyloxy, 3-butenyloxy, 2-pentenyloxy, 1-pentenyloxy,

3-pentenyloxy, 4-pentenyloxy, 1,3-butadienyloxy, 1,3-pentadienyloxy, 2-pentene

4-yloxy, 2-hexenyloxy, 1-hexenyloxy, 5-hexenyloxy, 3-hexenyloxy, 4-hexenyloxy, 3,3-dimethyl-1-propenyloxy, 2-ethyl-1-propenyloxy, 1,3,5-hexatrienyloxy, 1,3-hexadie-

nyloxy, and 1,4-hexadienyloxy.

Examples of lower pyridyl alkoxy groups optionally substituted on the pyridine ring with one or more lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more halogen atoms include: pyridylalkoxy groups wherein the alkoxy moiety is a group Ci-e

branched or linear alkoxy optionally substituted on the pyridine ring with one to three linear and / or branched C1-6 alkyl groups described above, each alkyl substituent optionally being substituted with one to three halogen atoms;

such as [(2-, 3-, or 4-) pyridyl] methoxy, 2 - [(2-, 3-, or 4-) pyridyl] ethoxy, 1 - [(2-, 3-, or 4 -) pyridyl] ethoxy, 3 - [(2-, 3-, or 4-) pyridyl] propoxy, 4 - [(2-, 3-, or 4-) pyridyl] butoxy, 5 - [(2-, 3 -, or 4-) pyridyl] pentyloxy, 6 - [(2-, 3-, or 4-) pyridyl] hexyloxy, 1,1-dimethyl-2 - [(2-, 3-, or 4-) pyridyl] ethoxy, 2-methyl-3 - [(2-, 3-, or 4-) pyridyl] propoxy, [2-trifluoromethyl- (3-, 4-, 5-, or 6-) pyridyl] methoxy, [ 2-methyl- (3-, 4-, 5-, or 6-) pyridyl] methoxy, [2,4-dimethyl- (3-, 5-, or 6-) pyridyl] methoxy, [2,4,6 - trimethyl- (3- or 5-) pyridyl] methoxy, [2-trifluoromethyl-4-methyl- (3-, 5-, or 6-) pyridyl] methoxy, 2- [3-ethyl- (2- 4-, 5-, or 6-) pyridyl] ethoxy, 3- [4-n-propyl- (2- or 3-) pyridyl] propoxy, 4- [3-n-butyl- (2-, 4-, 5-, or 6-) pyridyl] butyl, 5- [3-trifluoromethyl- (2-, 4-, 5-, or 6-) pyridyl] pentyloxy, 6- [2-n-pentyl- (3-, 4-, 5-, or 6-) pyridyl] hexyloxy, and [2-n-hexyl- (3-, 4-, 5-, or 6-) pyridyl] methoxy.

Examples of lower alkynyloxy groups include straight and branched C 2-6 alkynyloxy groups such as ethinyloxy, 2-propynyloxy, 2-butynyloxy,

3-Butynyloxy, 1-methyl-2-propynyloxy, 2-pentinyloxy, and 2-hexynyloxy.

Examples of lower phenyl alkynyloxy groups include phenylalkyloxy groups wherein the alkynyloxy moiety is a straight or branched C 2-6 alkynyloxy group such as 2-phenylethynyloxy, 3-phenyl-2-propynyloxy, 4-phenyl-2-butynyloxy, 4-phenyl-3-butynyloxy, 3-phenyl-1-methyl-2-propynyloxy, 5-phenyl-2-pentynyloxy, and 6-phenyl-2-hexynyloxy.

Examples of phenyl lower alkenyloxy groups include phenylalkenyloxy groups containing one to three double bonds wherein the alkenyloxy moiety is a straight or branched C 2-6 alkenyloxy group, such as styryloxy, 3-phenyl-1-propenyloxy, 3-phenyl-1 -methyl-1-propenyloxy, 3-phenyl-2-methyl-1-propenyloxy, 3-phenyl-2-propenyloxy, 4-phenyl-2-butenyloxy, 4-phenyl-1-butenyloxy, 4-phenyl-3 -butyloxy,

4-phenyl-2-pentenyloxy, 5-phenyl-1-pentenyloxy, 5-phenyl-3-pentenyloxy, 5-phenyl-4-pentenyloxy, 4-phenyl-1,3-butadienyloxy, 5-phenyl-1,3- pentadienyloxy, 5-phenyl-2-penten-4-yloxy, 6-phenyl-2-hexenyloxy, 6-phenyl-1-hexenyloxy, 6-phenyl-5-hexenyloxy,

6-phenyl-3-hexenyloxy, 6-phenyl-4-hexenyloxy, 3-phenyl-3,3-dimethyl-1-propenyloxy, 3-phenyl-2-ethyl-1-propenyloxy, 6-phenyl-1,3, 5-hexathienyloxy, 6-phenyl-1,3-hexadienyloxy, and 6-phenyl-1,4-hexadienyloxy. Examples of lower furyl alkoxy groups optionally substituted on the furan ring with one or more lower alkoxycarbonyl groups include: furylalkoxy groups wherein the alkoxy moiety is a branched or straight C1-6 alkoxy group optionally substituted on the furan ring with a to three alkoxycarbonyl groups described above wherein the alkoxy moiety is a straight and branched C1-6 alkoxy group;

such as [(2- or 3-) furylmethoxy, 2 - [(2- or 3-) furyl] ethoxy, 1 - [(2- or 3-) furyljetoxy, 3 - [(2- or 3-) furyl] propoxy, 4 - [(2- or 3-) furyl] butoxy, 5 - [(2- or 3-) furyl] pentyloxy, 6 - [(2- or 3-) furyl] hexyloxy, 1,1-dimethyl-2- [(2- or 3-) furyl] ethoxy, 2-methyl-3 - [(2- or 3-) furyl] propoxy, [2-ethoxycarbonyl- (3-, 4-, or 5-) furyl] methoxy, [2-methoxycarbonyl- (3-, 4-, or 5-) furyl] methoxy, [3-n-propoxycarbonyl- (2-, 4-, or 5-) furyl] methoxy, [2-n-butoxycarbonyl- ( 3-, 4-, or 5-) furyl] methoxy, [3-n-pentyloxycarbonyl- (2-, 4-, or 5-) furyl] methoxy, [2-n-hexyloxycarbonyl- (3-, 4 -, or 5-) furylmethoxy, [2,3-diethoxycarbonyl- (4- or 5-) furyl] methoxy, 2,3,4-trimethoxycarbonyl-5-furyl) methoxy, 2- [3-n-propoxycarbonyl - (2-, 4-, or 5-) furyl] ethoxy, 3- [2-n-butoxycarbonyl- (3-, 4-, or 5-) furyl] propoxy, 4- [3-n-pentyloxycarbonyl- ( 2-, 4-, or 5-) furyl] butoxy, 5- [2-n-hexyloxycarbonyl- (3-, 4-, or 5-) furyl] pentyloxy, and 6- [2-n-hexyloxycarbonyl- (3-, 4-, or 5-) furyl] hexyloxy.

Examples of lower tetrazolyl alkoxy groups optionally substituted on the tetrazol ring with a member selected from the group consisting of a phenyl group, lower phenyl alkyl groups, and lower cycloalkyl alkyl groups include:

tetrazolylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group optionally substituted on the tetrazole ring with a member selected from the group consisting of a phenyl group, the above-described phenylalkyl groups wherein the alkyl moiety is a group Straight or branched C1-6 alkyl, and the above C3-8 cycloalkyl alkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group;

such as [(1- or 5-) tetrazolyl] methoxy, 2 - [(1- or 5-) tetrazolyl] ethoxy, 1 - [(1- or 5-) tetrazolyl] ethoxy, 3 - [(1- or 5 -) tetrazolyl] propoxy, 4 - [(1- or 5-) tetrazolyl] butoxy, 5 - [(1- or 5-) tetrazolyl] pentyloxy, 6 - [(1- or 5-) tetrazolyl] hexyloxy, 1,1-dimethyl-2 - [(1- or 5-) tetrazolyl] ethoxy, 2-methyl-3 - [(1- or 5-) tetrazolyl] propoxy, (1-benzyl-5-tetrazolyl) methoxy, ( 1-phenyl-5-tetrazolyl) methoxy, (1-cyclohexylmethyl-5-tetrazolyl) methoxy, [5- (2-phenylethyl) -1-tetrazolyl] methoxy, [1- (1-phenylethyl) -5-tetrazolyl ] methoxy, [1- (3-phenylpropyl) -5-tetrazolyl] methoxy, [5- (4-phenylbutyl) -1-tetrazolyl] methoxy, [1- (5-phenylpentyl) -5-tetrazolyl] methoxy, [1 - (6-phenylexyl) -5-tetrazolyl] methoxy, [5- (2-cycloethylethyl) -1-tetrazolyl] methoxy, [1- (1-cyclopropylethyl) -5-tetrazolyl] methoxy, [1- (3-cyclobutylpropyl ) -5-tetrazolyl] methoxy, [5- (4-cyclopentylbutyl) -1-tetrazolyl] methoxy, [1- (5-icloeptylpentyl) -5-tetrazolyl] methoxy, [1- (6-cyclooctylhexyl) -5-tetrazolyl ] methoxy, 2- (1-phenyl-5-tetrazoli 1) ethoxy, 3- (1-cycloexylmethyl-5-tetrazolyl) propoxy, 4- [5- (2-phenylethyl) -1-tetrazolyl] butoxy, 5- (1-benzyl-5-tetrazolyl) pentyloxy, 6 - (1-phenyl-5-tetrazolyl) hexyloxy, and 1- (1-cycloexylmethyl-5-tetrazolyl) ethoxy.

Examples of phenyl ring optionally substituted phenyl groups with one or more lower alkyl groups include optionally substituted phenyl ring phenyl groups having one to three linear and / or branched C1-6 alkyl groups, such as phenyl, 2-methylphenyl , 3-methylphenyl, 4-methylphenyl, 2-ethylphenyl, 3-ethylphenyl, 4-ethylphenyl, 4-isopropylphenyl, 3-n-butylphenyl, 4-n-pentylphenyl, 4-n-hexylphenyl, 3,4-dimethylphenyl 3,4-diethylphenyl, 2,4-dimethylphenyl, 2,5-dimethylphenyl, 2,6-dimethylphenyl, and 3,4,5-trimethylphenyl.

Examples of 1,2,4-oxadiazolyl lower alkoxy groups optionally substituted on the 1,2,4-oxadiazole ring with a phenyl group, the phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups, include:

1,2,4-oxadiazolylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group optionally substituted on the 1,2,4-oxadiazole ring with one of the above described phenyl groups optionally substituted on the phenyl ring with one to three straight and / or branched C1-6 alkyl groups;

such as [(3- or 5-) 1,2,4-oxadiazolyl] methoxy, 2 - [(3- or 5-) 1,2,4-oxadiazolyl] ethoxy, 1 - [(3- or 5-) 1,2,4-oxadiazolyl] ethoxy, 3 - [(3- or 5-) 1,2,4-oxadiazolyl] propoxy, 4 - [(3- or 5-) 1,2,4-oxadiazolyl] butoxy, 5 - [(3- or 5-) 1,2,4-oxadiazolyl] pentyloxy, 6 - [(3- or 5-) 1,2,4-oxadiazolyl] hexyloxy, 1,1-dimethyl-2 - [( 3- or 5-) 1,2,4-oxadiazolyl] ethoxy, 2-methyl-3 - [(3- or 5-) 1,2,4-oxadiazolyl] propoxy, [3- (4-tert-butylphenyl) -5-1,2,4-oxadiazolyl] methoxy, [3- (3-methylphenyl) -5-1,2,4-oxadiazolyl] methoxy, [5- (2-ethylphenyl) -3-1,2 , 4-oxadiazolyl] methoxy, [3- (4-n-propylphenyl> -5,21,2,4-oxadiazolyl] methoxy, [5- (3-n-pentylphenyl) -3-1,2,4-oxadiazolyl ] methoxy, [3- (2-n-hexitphenyl) -5-1,2,4-oxadiazolyl] methoxy, [3- (2,4-dimethylphenyl) -5-1,2,4-oxadiazolyl] methoxy , [3- (2,3,5-trimethylphenyl) -5-1,2,4-oxadiazolyl] methoxy, 2- [3- (4-tert-butylphenyl) -5-1,2,4-oxadiazolyl] ethoxy , 1- [3- (3-methylphenyl) -5-1,2,4-oxadiazolyl] ethoxy, 3- [5- (2-ethylphenyl) -3-1,2,4-oxadiazolyl] propoxy, 4 - [3- (4 - /> p ropylphenyl) -5-1,2,4-oxadiazolyl] butoxy, 5- [5- (3-n-pentylphenyl) -3-1,2,4-oxadiazolyl] pentyloxy, 6- [3- (2-n- hexylphenyl) -5-1,2,4-oxadiazolyl] hexyloxy, 2- [3- (2,4-dimethylphenyl) -5-1,2,4-oxadiazolyl] ethoxy and 1- [3- (2,3, 5-trimethylphenyl) -5-1,2,4-oxadiazolyl] ethoxy.

Examples of lower isoxazolyl alkoxy groups optionally substituted on the isoxazole ring with one or more lower alkyl groups include: isoxazolylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group, optionally substituted on the isoxazole ring with one or two C1 groups Linear and / or branched alkyls described above; such as [(3-, 4-, or 5-) isoxazolyl] methoxy, 2 - [(3-, 4-, or 5-) isoxazolyl] ethoxy, 1 - [(3-, 4-, or 5-) isoxazolyl] ethoxy, 3 - [(3-, 4-, or 5-) isoxazolyl] propoxy, 4 - [(3-, 4-, or 5-) isoxazolyl] butoxy, 5 - [(3-, 4-, or 5-) isoxazolyl] pentyloxy, 6 - [(3-, 4-, or 5-) isoxazolyl] hexyloxy, 1,1-dimethyl-2 - [(3-, 4-, or 5-) isoxazolyl] ethoxy, 2-methyl-3 - [(3-, 4-, or 5-) isoxazolyl] propoxy, (3,5-dimethyl-4-isoxazolyl) methoxy, [3-methyl- (4- or 5-) isoxazolyl] methoxy, [ 3-ethyl- (4- or 5-) isoxazolyl] methoxy, [4-n-propyl- (3- or 5-) isoxazolyl] methoxy, [5-n-butit- (3- or 4-) isoxazolyl] methoxy , [3-n-pentyl- (4- or 5-) isoxazolyl] methoxy, [4-n-hexyl- (3- or 5-) isoxazolyl] methoxy, 2- [3-methyl- (4- or 5-) iso - xazolyl] ethoxy, 1- [3-ethyl- (4- or 5-) isoxazolyl] ethoxy, 3- [4-n-propyl- (3- or 5-) isoxazolyl] propoxy, 4- [5- n-butyl- (3- or 4-) isoxazolyl] butoxy, 5- [3-n-pentyl- (4- or 5-) isoxazolyl] pentyloxy, and 6- [4-n-hexyl- (3- or 5-) isoxazolyl] hexyloxy.

Examples of 1,3,4-oxadiazolyl lower alkoxy groups optionally substituted on the 1,3,4-oxadiazole ring with a phenyl group, the phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups include :

1,3-oxadiazolylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group optionally substituted on the 1,3,4-oxadiazole ring with one of the above described phenyl groups optionally substituted on the phenyl ring with one to three straight and / or branched C1-6 alkyl groups;

such as [(2- or 5-) 1,3,4-oxadiazolyl] methoxy, 2 - [(2- or 5-) 1,3,4-oxadiazolyl] ethoxy, 1 - [(2- or 5-) 1,3,4-oxadiazolyl] ethoxy, 3 - [(2- or 5-) 1,3,4-oxadiazolyl] propoxy, 4 - [(2- or 5-) 1,3,4-oxadiazolyl] butoxy, 5 - [(2- or 5-) 1,3,4-oxadiazolyl] pentyloxy, 6 - [(2- or 5-) 1,3,4-oxadiazolyl] hexyloxy, 1,1-dimethyl-2 - [( 2- or 5-) 1,3,4-oxadiazolyl] ethoxy, 2-methyl-3 - [(2- or 5-) 1,3,4-oxadiazolyl] propoxy, [2- (4-tert-butylphenyl) -5-1,3,4-oxadiazolyl] methoxy, [2- (4-methylphenyl) -5-1,3,4-oxadiazolyl] methoxy, [5- (2-ethylphenyl) -2-1,3,4 -oxadiazolyl] methoxy, [2- (4-n-propylphenyl) -5,31,4-oxadiazolyl] methoxy, [5- (3-n-pentylphenyl) -2-1,3,4-oxadiazolyl] methoxy , [2- (2-n-hexylphenyl) -5-1,3,4-oxadiazolyl] methoxy, [2- (2,4-dimethylphenyl) -5-1,3,4-oxadiazolyl] methoxy, [ 2- (2,3,5-trimethylphenyl) -5-1,3,4-oxadiazoyl] methoxy, 2- [2- {A-tert-butylphenyl) -5-1,3,4-oxadiazolyl] ethoxy, 1 - [2- (3-methylphenyl) -5-1,3,4-oxadiazolyl] ethoxy, 3- [5- (2-ethylphenyl) -2-1,3,4-oxadiazolyl] propoxy, 4- [ 2- (4-n-propi 1-phenyl) -5-1,3,4-oxadiazolyl] butoxy, 5- [5- (3-n-pentylphenyl) -2-1,3,4-oxadiazolyl] pentyloxy, 6- [2- (2-r? -hexylphenyl) -5-1,3,4-oxadiazolyl] hexyloxy, 2- [2- (2,4-dimethylphenyl) -5-1,3,4-oxadiazolyljetoxy, and 1- [2- (2,3, 5-trimethylphenyl) -5-1,3,4-oxadiazolyl] ethoxy.

Examples of lower alkanoyl alkoxy groups include alkanoyl alkoxy groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group and the alkoxy moiety is a branched or straight C1-6 alkoxy group such as acetylmethoxy, propionylmethoxy, 2- acetyloxy, 2-propionyloxy, 1-acetyloxy, 3-acetylpropoxy, 3-propionylpropoxy, 4-acetylbutoxy, 5-butyrylpentyloxy, 6-pentanoylhexyloxy, 1,1-dimethyl-2-hexanoyloxy, 2-methyl-3-acetylpropoxy, 2- pentanoyloxy, and hexanoylmethoxy. Examples of optionally substituted phenyl groups on the ring

phenyl with one or more halogen atoms include phenyl groups optionally substituted on the phenyl ring with one to three halogen atoms, such as phenyl, 4-fluorophenyl, 2,5-difluorophenyl, 2,4-difluorophenyl, 3,4- difluorophenyl, 3,5-difluorophenyl, 2,6-difluorophenyl, 2-chlorophenyl, 3-chlorophenyl, 4-chlorophenyl, 2,3-dichlorophenyl, 2,4-dichlorophenyl, 2,5-dichlorophenyl, 3,4- dichlorophenyl, 2,6-dichlorophenyl, 3-fluorophenyl, 2-fluorophenyl, 3-bromophenyl, 4-iodophenyl, 2-bromophenyl, 4-bromophenyl, 3,5-dichlorophenyl, 2,4,6-trifluorophenyl, 3,4-difluorophenyl, 2-iodophenyl, 3-iodophenyl, 4-iodophenyl, 2,3-dibromophenyl, 2,4-diiodophenyl, and 2,4,6-trichlorophenyl.

Examples of lower thiazolyl alkoxy groups optionally substituted on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and one phenyl group, each phenyl substituent optionally being substituted on the phenyl ring with one or more atoms halogen, include:

thiazolylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group, optionally substituted on the triazole ring with one or two members selected from the group consisting of the above described linear and branched C1-6 alkyl groups and optionally phenyl groups substituted on the phenyl ring with one to three halogen atoms;

such as [(2-, 4-, or 5-) thiazolyl] methoxy, 2 - [(2-, 4-, or 5-) thiazolyl] ethoxy, 1 - [(2-, 4-, or 5 -) thiazolyl] ethoxy, 3 - [(2-, 4-, or 5-) thiazolyl] propoxy, 4 - [(2-, 4-, or 5-) thiazolyl] butoxy, 5 - [(2-, 4-, or 5-) thiazolyl] pentyloxy, 6 - [(2-, 4-, or 5-) thiazolyl] hexyloxy, 1,1-dimethyl-2 - [(2-, 4-, or 5-) thiazolyl] ethoxy, 2-methyl-3 - [(2-, 4-, or 5-) thiazolyl] propoxy, [2-phenyl- (4- or 5-) thiazolylmethoxy, [2- (4-chlorophenyl) -4-methyl Thiazolyl] methoxy, [2- (3-bromophenyl) - (4- or 5-) thiazolyl] methoxy, [2- (2-fluorophenyl) - (4- or 5-) thiazolyl] methoxy, [2- (3 , 4-dichlorophenyl) - (4- or 5-) thiazolyl] methoxy, [2- (2,4,6-trifluorophenyl) - (4- or 5-) thiazolylmethoxy, [2-methyl- (4- or 5- ) thiazolylmethoxy, 2- [2-ethyl- (4- or 5-) thiazolyl] methoxy, 2- [4-phenyl- (2- or 5-) thiazolyl] ethoxy, 3- [5-n-propyl- (2 - or 4-) thiazolyl] propoxy, 4- [4-n-butyl- (2- or 5-) thiazolyl] butoxy, 5- [2-n-pentyl- (4- or 5-) thiazolyl] pentyloxy, 6- [5- n-hexyl- (2- or 4-) thiazolylhexyloxy, [2,4-dimethyl-5-thiazolylmethoxy, and [2,4-diphenyl] 1-5-thiazolyl] methoxy. Examples of optionally substituted benzoyl groups on the

phenyl ring having one or more halogen atoms include optionally substituted benzoyl groups on the phenyl ring having one to three halogen atoms such as benzoyl, 4-fluorobenzoyl, 2,5-difluorobenzoyl, 2,4-difluorobenzoyl, 3 , 4-difluorobenzoyl, 3,5-difluorobenzoyl, 2,6-difluorobenzoyl, 2-chlorobenzoyl, 3-chlorobenzoyl, 4-chlorobenzoyl, 2,3-dichlorobenzoyl, 2,4-dichlorobenzoyl, 2,5-dichlorobenzoyl, 3,4 -dichlorobenzoyl, 2,6-dichlorobenzoyl, 3-fluorobenzoyl, 2-fluorobenzoyl, 3-bromobenzoyl, 4-iodobenzoyl, 2-bromobenzoyl, 4-bromobenzoyl, 3,5-dichlorobenzoyl, 2,4,6-trifluorobenzoyl, 2-iodobenzyl , 3-iodobenzoyl, 4-iodobenzoyl, 2,3-dibromobenzoyl, 2,4-diiodobenzoyl, and 2,4,6-trichlorobenzoyl.

Examples of piperidinyloxy groups optionally substituted on the piperidine ring with one or more benzoyl groups, each benzoyl substituent optionally being substituted on the phenyl ring with one or more halogen atoms, include:

piperidinyloxy groups optionally substituted on the piperidine ring with one to three benzoyl groups described above, each benzoyl substituent optionally being substituted on the phenyl ring with one to three halogen atoms;

such as (1-, 2-, 3-, or 4-) piperidinyloxy, 1- (4-chlorobenzoyl) - (2-, 3-, or 4-piperidinyloxy, 1- (3-bromobenzoyl) - (2-, 3-, or 4-) piperidinyloxy, 1-benzoyl- (2-, 3-, or 4-) piperidinyloxy, 1- (2-fluorobenzoyl) - (2-, 3-, or 4-) piperidinyloxy, 1- ( 2,4-dichlorobenzoyl) - (2-, 3-, or 4-) piperidinyloxy, 1- (2,4,6-trifluorobenzoyl) - (2-, 3-, or 4-) piperidinyloxy, 2- (3- chlorobenzoyl) - (1-, 3-, or 4-) piperidinyloxy, 3- (2-chlorobenzoyl) - (1-, 2-, or 4-) piperidinyloxy, 4- (2,3-dibromobenzoyl) - (1- , 2-, or 3-) piperidinyloxy, 1,2-dibenzoyl- (3- or 4-) piperidinyloxy, and 1,2,4-tribenzoyl-3-piperidinyloxy.

Examples of lower alkoxy thienyl groups include thienylalkoxy groups.

where the alkoxy moiety is a straight or branched C1-6 alkoxy group such as [(2- or 3-) thienyl] methoxy, 2 - [(2- or 3-) thienyl] ethoxy, 1 - [( 2- or 3-) thienyl] ethoxy, 3 - [(2- or 3-) thienyl] propoxy, 4 - [(2- or 3-) thienyl] butoxy, 5 - [(2- or 3-) thienyl] pentyloxy, 6 - [(2- or 3-) thienyl] hexyloxy, 1,1-dimethyl-2 - [(2- or 3-) thienyl] ethoxy, and 2-methyl-3 - [(2 - or 3-) thienyl] propoxy.

Examples of lower phenylthio alkoxy groups include phenylthioalkoxy groups wherein the alkoxy moiety is a branched or alkaryl C1-6 alkoxy group such as phenylthiomethoxy, 2-phenylthioethoxy, 1-phenylthioethoxy, 3-phenylthiopropoxy, 4-phenylthiobutoxy, 5-phenylthiopentyloxy, 6-phenylthioexyloxy, 1,1-dimethyl-2-phenylthioethoxy, and 2-methyl-3-phenylthiopropoxy.

Examples of carbamoyl-substituted lower alkoxy groups optionally substituted with one or more lower alkyl groups include: branched and branched carbamoyl substituted C1-6 alkoxy groups optionally substituted by carbamoyl group having one or two straight C1-6 alkyl groups and / or branched;

such as carbamoylmethoxy, 2-carbamoyloxy, 1-carbamoyloxy, 3-carbamoylpropoxy, 4-carbamoylbutoxy, 5-carbamoylpentyloxy, 6-carbamoylhexyloxy, 1,1-dimethyl-2-carbamoyloxy, 2-methyl-3-carbamoylpropoxy, methylcarbamide moylmethoxy, 1-ethylcarbamoyloxy, 2-n-propylcarbamoyloxy, 3-isopropylcarbamoylpropoxy, 4-n-butylcarbamoylbutoxy, 5-n-pentylcarbamoylpentyloxy, 6-n-hexylcarbamoylhexylcarbamoylpropylcarbamoyl ethyl (N-propylcarbamoyl) methoxy, and 2- (N-methyl-N-hexylcarbamoyl) ethoxy.

Examples of lower benzoyl alkoxy groups include benzoylalkoxy groups wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group such as benzoylmethoxy, 2-benzoyloxy, 1-benzoyloxy, 3-benzoylpropoxy, 4-benzoyl butoxy, 5-benzoylpentyloxy, 6-benzoylhexyloxy, 1,1-dimethyl-2-benzoyloxy, and 2-methyl-3-benzoylpropoxy.

Examples of lower alkoxy pyridylcarbonyl groups include pyridylcarbonylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group such as [(2-, 3-, or 4-) pyridylcarbonyl] methoxy, 2 - [(2- , 3-, or 4-) pyridylcarbonyl] ethoxy, 1 - [(2-, 3-, or 4-) pyridylcarbonyl] ethoxy, 3 - [(2-, 3-, or 4-) pyridylcarbonyl] propoxy, 4- [(2-, 3-, or 4-) pyridylcarbonyl] butoxy, 5 - [(2-, 3-, or 4-) pyridylcarbonyl] pentyloxy, 6 - [(2-, 3-, or 4-) pyridylcarbonyl] hexyloxy, 1,1-dimethyl-2 - [(2-, 3-, or 4-) pyridylcarbonyl] ethoxy, and 2-methyl-3 - [(2-, 3-, or 4-) pyridylcarbonyl] propoxy .

Examples of lower imidazolyl alkoxy groups optionally

ring substituted on the imidazole with one or more lower alkyl phenyl groups include:

imidazolylalkoxy groups wherein the alkoxy moiety is a branched or linear C 1-6 alkoxy group, optionally substituted on the imidazole ring with one to three phenylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group;

such as [(1-, 2-, 4-, or 5-) imidazolyl] methoxy, 2 - [(1-, 2-, 4-, or 5-) imidazolyl] ethoxy, 1 - [(1-, 2-, 4-, or 5-) imidazolyl] ethoxy, 3 - [(1-, 2-, 4-, or 5-) imidazolyl] propoxy, 4 - [(1-, 2-, 4-, or 5-) imidazolyl] butoxy , 5 - [(1-, 2-, 4-, or 5-) imidazolyl] pentyloxy, 6 - [(1-, 2-, 4-, or 5-) imidazolyl] hexyloxy, 1,1-dimethyl -2 - [(1-, 2-, 4-, or 5-) imidazolyl] ethoxy, 2-methyl-3 - [(1-, 2-, 4-, or 5-) imidazolyl] propoxy, [1- benzyl- (2-, 4-, or 5-) imidazolyl] methoxy, [1- (2-phenylethyl) - (2-, 4-, or 5-) imidazolinylmethoxy, 2- [2- (3-phenylpropyl ) - (1-, 4-, or 5-) imidazolyl] ethoxy, 3- [4- (4-phenylbutyl) - (1-, 2-, or 5-) imidazolyl] propoxy, 5- [4- (5 (phenyl, pentyl) - (1-, 2-, or 4-) imidazolyl] pentyloxy, 6- [1- (6-phenylexyloxy) - (2-, 4-, or 5-) imidazolyl] hexoxy, [1,2- dibenzyl- (4- or 5-) imidazolyl] methoxy, and [1,2,4-tribenzyl-5-imidazolyl] methoxy. Examples of lower phenoxy alkoxy groups include phenoxy groups.

alkoxy wherein the alkoxy moiety is a branched or straight alkoxy C1-6 group such as phenoxymethoxy, 2-phenoxyethoxy, 1-phenoxyethoxy, 3-phenoxypropoxy, 4-phenoxypentyloxy, 6-phenoxyhexyloxy, 1,1-dimethyloxy 2-phenoxyethoxy, and 2-methyl-3-phenoxypropoxy. Examples of phenyl alkoxy-substituted lower alkoxy groups

Lower alkoxy groups include phenylalkoxy substituted alkoxy groups wherein each of the two alkoxy moieties is a branched or straight C1-6 alkoxy group such as phenylmethoxymethoxy, 2- (phenylmethoxy) ethoxy, 1- (phenylmethoxy) ethoxy, 3- (phenylmethoxy) propoxy 4- (phenylmethoxy) butoxy, 5- (phenylmethoxy) pentyloxy, 6- (phenylmethoxy) hexyloxy, 1,1-dimethyl-2- (phenylmethoxy) ethoxy, 2-methyl-3- (phenylmethoxy) propoxy, 1- (2-phenylethoxy) ethoxy, 2- (1-phenylethyloxy) ethoxy, 3- (3-phenylpropoxy) propoxy, 4- (4-phenylbutoxy) butoxy, 5- (5-phenylpentyloxy) pentyloxy, 6- (6- phenylexyloxy) hexyloxy, (1,1-dimethyl-2-phenylethyloxy) methoxy, and 3- (2-methyl-3-phenylpropoxy) propoxy.

Examples of lower isoindolinyl alkoxy groups optionally substituted on the isoindoline ring with one or more oxo groups include:

isoindolinylalkoxy groups wherein the alkoxy moiety is a branched or linear C1-6 alkoxy group, optionally substituted on the isoindoline ring with one or two oxo groups;

such as [(1-, 2-, 4-, or 5-) isoindolinyl] methoxy, 2 - [(1-, 2-, 4-, or 5-) isoindolinyl] ethoxy, 1 - [(1-, 2 -, 4-, or 5-) isoindolinyl] ethoxy, 3 - [(1-, 2-, 4-, or 5-) isoindolinyl] propoxy, 4 - [(1-, 2-, 4-, or 5- ) isoindolinyl] butoxy, 5 - [(1-, 2-, 4-, or 5-) isoindolinyl] pentyloxy, 6 - [(1-, 2-, 4-, or 5-) isoindolinyl] hexyloxy, 1,1-dimethyl -2 - [(1- 2-, 4-, or 5-) isoindolinyl] ethoxy, 2-methyl-3 - [(1-, 2-, 4-, or 5-) isoindolinyl] propoxy,

3- [1,3-dioxo- (2-, 4-, or 5-) isoindolinyl] propoxy, [1-oxo- (2-, 3-, 4-, 5-, 6-, or 7-) isoindolinyl ] methoxy, 2- [1,3-dioxo- (1-, 4-, or 5-) isoindolinyl] ethoxy, 4- [1-oxo- (2-, 3-, 4-, 5-, 6-, or 7-) isoindolinyl] butoxy, 5- [1,3-dioxo- (1-, 4-, or 5-) isoindolinyl

phenyl] pentyloxy, and 6- [1-oxo- (2-, 3-, 4-, 5-, 6-, or 7-) isoindolinyl] hexyloxy.

Examples of lower alkoxy groups optionally substituted with one or more halogen atoms include straight and branched C1-6 alkoxy groups optionally substituted with one to three halogen atoms, such as, in addition to lower alkoxy, trifluoromethoxy, trichloromethoxy, chloromethoxy, bromomethoxy, fluoromethoxy, iodomethoxy, difluoromethoxy, dibromomethoxy, 2-chloroethoxy, 2,2,2-trifluoroethoxy, 2,2,2-trichloroethoxy, 3-chloropropoxy, 2,3-dichloropropoxy, 4,4,4-trichlorobutoxy, 4-Fluorobutoxy, 5-chloropentyloxy, 3-chloro-2-methylpropoxy, 5-bromoexyloxy, and 5,6-dibromoexyloxy described above.

Examples of lower alkanoyl groups include straight and branched C 1-6 alkanoyl groups such as formyl, acetyl, propionyl, butyryl, isobutyryl, pentanoyl, tert-butylcarbonyl, and hexanoyl.

Examples of nitro groups optionally substituted with one or more lower alkanoyl groups include amino groups optionally substituted with one or two straight and / or branched C1-6 alkanoyl groups, such as amino, formylamino, acetylamino, propionylamino, butyrylamino, isobutyrylamino pentanoylamino, tert-butylcarbonylamino, hexanoylamino, N, N-diacylamino, and acetyl - propionylamino.

Examples of phenyl lower alkyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups optionally substituted with one or more halogen atoms; a phenyl group; lower alkoxycarbonyl groups; a phenoxy group; lower alkylthio groups; lower alkylsulfonyl groups; phenyl lower alkoxy groups; and optionally substituted nitro groups with one or more lower alkanoyl groups include: mono- and di-phenylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the one to three membered phenyl ring selected from the group consisting of the halogen atoms described above; the linear and branched C1-6 alkyl groups described above optionally substituted with one to three halogen atoms; the linear and branched C1-6 alkoxy groups described above optionally substituted with one to three halogen atoms; a phenyl group; the alkoxycarbonyl groups described above wherein the alkoxy moiety is a straight and branched C1-6 alkoxy group; a phenoxy group, the linear and branched C1-6 alkylthio groups described above; the linear and branched C1-6 alkylsulfonyl groups described above; phenylalkoxy groups described above wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group; and the above-described amino groups optionally substituted by one or two straight and / or branched C1-6 alkanoyl groups;

such as benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenylexyl, 2-methyl-3-phenylpropyl, 1, 1-Dimethyl-2-phenylethyl, 1,1-diphenylmethyl, 2,2-diphenylethyl, 3,3-diphenyl-propyl, 1,2-diphenylethyl, 4-chlorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 3-fluorobenzyl robenzyl, 4-fluorobenzyl, 2,3-dichlorobenzyl, 2,4,6-trifluorobenzyl, 3-trifluoromethylbenzyl, 4-trifluoromethylbenzyl, 2-methylbenzyl, 3-methylbenzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 2,4-dimethylbenzyl, 2,4,6-trimethylbenzyl, 2-phenylbenzyl, 4-phenylbenzyl, 2,4-diphenylbenzyl, 2,4,6-triphenylbenzyl, 2-trifluoromethoxybenzyl, 3-trifluoromethoxybenzyl, 4- trifluoromethoxybenzyl, 2-methoxybenzyl, 3-methoxybenzyl, 4-methoxybenzyl, 3,4-dimethoxybenzyl, 3,4,5-trimethoxybenzyl, 4-methoxycarbonylbenzyl, 3-ethoxycarbonylbenzyl, 2-n-propoxycarbonylbenzyl, 2 4-dimethoxycarbonylbenzyl, 2,4,6-trimethoxycarbonylbenzyl, 4-tert-butoxycarbonylbenzyl, 3-phenoxyb Enzyme, 2-phenoxybenzyl, 4-phenoxybenzyl, 3,4-diphenoxybenzyl, 3,4,5-triphenoxybenzyl, 4-methylthiobenzyl, 3-methylthiobenzyl, 2-methylthiobenzyl, 2,4-dimethylthiobenzyl, 2,4,6-trimethylthiobenzyl, 4-methylsulfonylbenzyl, 3-methylsulfonylbenzyl, 2-methylsulfonylbenzyl, 3,4-dimethylsulfonylbenzyl, 3,4,5-trimethylsulfonylbenzyl, 4-benzyloxybenzyl, 2-benzyloxybenzyl, 2-benzyloxybenzyl, 2,4-dibenzyloxybenzyl, 2 4,6-tribenzyloxybenzyl, 4-methoxy-3-chlorobenzyl, 4- (N-acetylamino) benzyl, 3-aminobenzyl, 2-aminobenzyl, 4-aminobenzyl, 2,3-diaminobenzyl, 3,4,5-triaminobenzyl, and 4-methyl-3-fluorobenzyl.

Examples of lower alkyl naphthyl groups include naphthylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, such as [(1- or 2-) naphthyl] methyl, 1 - [(1- or 2 -) naphthyl] ethyl, 2 - [(1- or 2-) naphthyl] ethyl, 3 - [(1- or 2-) naphthyl] propyl, 2 - [(1- or 2-) naphthyl] propyl, 4 - [(1- or 2-) naphthyl] butyl, 5 - [(1- or 2-) naphthyl] pentyl, 4 - [(1- or 2-) naphthyl] pentyl, 6 - [(1- or 2-) naphthyl] hexyl, 2-methyl-3 - [(1- or 2-) naphthyl] propyl, and 1,1-dimethyl-2 - [(1- or 2-) naphthyljetyl.

Examples of lower furyl alkyl groups optionally substituted on the furan ring with one or more lower alkoxycarbonyl groups include: furylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the furan ring with one to three alkoxycarbonyl groups wherein the alkoxy moiety is a straight and branched C1-6 alkoxy group; such as [(2- or 3-) furyl] methyl, 2 - [(2- or 3-) furyl] ethyl, 1 - [(2- or 3-) furyl] ethyl, 3 - [(2- or 3-) furyl] propyl, 4 - [(2- or 3-) furyl] butyl, 5 - [(2- or 3-) furyl] pentyl, 6 - [(2- or 3-) furyl] hexyl, 1,1-dimethyl-2 - [(2- or

3-) furyl] ethyl, 2-methyl-3 - [(2- or 3-) furyl] propyl, [5-ethoxycarbonyl- (2-, 3-, or 4-) furyl] methyl, [5- methoxycarbonyl- (2-, 3-, or 4-) furyl] methyl, [2-n-propoxycarbonyl- (3-,

4-, or 5-) furyl] methyl, [3-tert-butoxycarbonyl- (2-, 4-, or 5-) furyl] methyl, [4- / 7-pentyloxycarbonyl- (2-, 3-, or 5 -) furyl] methyl, [2-n-hexyloxycarbonyl- (3-, 4-, or 5-)

furyl] methyl, [2,5-diethoxycarbonyl- (3- or 4-) furyl] methyl, and [2,4,5-triethoxycarbonyl-3-furyl] methyl.

Examples of phenyl groups optionally substituted on the phenyl ring with one or more lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more halogen atoms, include:

phenyl ring optionally substituted phenyl groups having one to three straight and / or branched C1-6 alkyl groups, each alkyl substituent optionally being substituted with one to three halogen atoms described above;

such as phenyl, 2-methylphenyl, 3-methylphenyl, 4-methylphenyl, 2-ethylphenyl, 3-ethylphenyl, 4-ethylphenyl, 4-isopropylphenyl, 3-n-butylphenyl, 4-n-pentylphenyl, 4-n- hexylphenyl, 3,4-dimethylphenyl, 3,4-diethylphenyl, 2,4-dimethylphenyl, 2,5-dimethylphenyl, 2,6-dimethylphenyl, 3,4,5-trimethylphenyl, 2-trifluoromethylphenyl, 3-trifluoromethylphenyl methylphenyl, 4-trifluoromethylphenyl, 3,5-difluoromethylphenyl, 2,4,6-tri (trifluoromethyl) phenyl, and 2-methyl-4-trifluoromethylphenyl.

Examples of optionally substituted lower alkyl thiazolyl groups

triazole ring having one or more members selected from the group consisting of lower alkyl groups and one phenyl group, each phenyl substituent optionally being substituted with one or more lower alkyl groups optionally substituted by halogen, include thiazolylalkyl groups wherein The alkyl moiety is a straight or branched C1-6 alkyl group. Such thiazoylalkyl groups include those optionally substituted on the triazole ring with one or two members selected from the linear and branched C1-6 alkyl groups described above and the above described phenyl groups optionally substituted on the phenyl ring with one to three C1-6 groups straight and / or branched alkyl, each alkyl substituent on the phenyl substituent optionally also being substituted with one to three halogen atoms. More specific examples of lower thiazolyl alkyl groups are [(2-, 4-, or 5-) thiazolyl] methyl, 2 - [(2-, 4-, or 5-) thiazolyljetyl, 1 - [(2-, 4- , or 5-) thiazolyl] ethyl, 3 - [(2-, 4-, or 5-) thiazolyl] propyl, 4 - [(2-, 4-, or 5-) thiazolyl] butyl, 5 - [(2 -, 4-, or 5-) thiazolyl] pentyl, 6 - [(2-, 4-, or 5-) thiazolyl] hexyl, 1,1-dimethyl-2 - [(2-, 4-, or 5- ) thiazolyl] ethyl, [2-methyl- (4- or 5-) thiazolyl] methyl, [2- (4-trifluoromethylphenyl) - [(4- or 5-) thiazolyl] methyl, 2- [4-ethyl- ( 2- or 5-) thiazolyl] ethyl, 1- [5- (3-methylphenyl) - (2- or 4-) thiazolyl] ethyl, 3- [5-isopropyl- (2- or 4-) thiazolyl] propyl, 4- [2- (2,4-dimethylphenyl) - (4- or 5-) thiazolyl] butyl, 5- [2- n -butyl- (4- or 5-) thiazolyl] pentyl, 6- [4- (2,4, 6-trimethylphenyl) - (2- or 5-) thiazolyl] hexyl, (2,4-dimethyl-5-thiazolyl) methyl, [2- (4-trifluoromethylphenyl) -4-phenyl-5-thiazolyl] methyl, and ( 2-phenyl-4-thiazolyl) methyl.

Examples of tetrazolyl lower alkyl groups optionally substituted on the tetrazol ring with one or more lower alkyl groups include: tetrazolylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the tetrazol ring with one or more C1 groups -6 linear and / or branched alkyls,

such as [(1- or 5-) tetrazolyl] methyl, 2 - [(1- or 5-) tetrazolyl] ethyl, 1 - [(1- or 5-) tetrazolyl] ethyl, 3 - [(1- or 5 -) tetrazolyl] propyl, 4 - [(1- or 5-) tetrazolyl] butyl, 5 - [(1- or 5-) tetrazolyl] pentyl, 6 - [(1- or 5-) tetrazolyl] butyl, 5- (1-methyl-5-tetrazolyl) pentyl, 6- (1-methyl-5-tetrazolyl) hexyl, (5-methyl-1-tetrazolyl) methyl,

2- (5-ethyl-1-tetrazolyl) hexyl, 1,1-dimethyl-2 - [(1- or 5-) tetrazolyl] ethyl, 2-methyl-3 - [(1- or 5-) tetrazolyl] propyl , (1-methyl-5-tetrazolyl) methyl, (1-ethyl-5-tetrazolyl) methyl, 2- (1-n-propyl-5-tetrazolyl) ethyl, 1- (1-n-butyl-5) tetrazolyl) ethyl, 3- (1-n-pentyl)

5-Tetrazolyl) propyl, 4- (1-n-hexyl-4-tetrazolyl) butyl, 3- (5-isopropyl-1-tetrazolyl) propyl, 4- (5-sec-butyl-1-tetrazolyl) butyl, 5 - (5-isopentyl-1-tetrazolyl) pentyl, and

6- (5-n-hexyl-1-tetrazolyl) hexyl.

Examples of benzothienyl lower alkyl groups optionally

Substituted in the benzothiophene ring with one or more halogen atoms include:

benzothienylalkyl groups wherein the alkyl moiety is a straight and branched C 1-6 alkyl group, optionally substituted on the benzothiophene ring having one to three halogen atoms;

such as [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] methyl, 2 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] ethyl, 1 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] ethyl, 3 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] propyl, 4 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] butyl, 5 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] pentyl, 6 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] hexyl, 1,1-dimethyl-2- [ (2-, 3-, 4-, 5-, 6-, or 7-) benzothenyl] ethyl, 2-methyl-3 - [(2-, 3-, 4-, 5-, 6-, or 7-) benzothienyl] propyl, [5-chloro- (2-, 3-,

4-, 6-, or 7-) benzothienyl] methyl, [4-bromo- (2-, 3-, 5-, 6-, or 7-) benzothenyl] methyl, [6-fluoro- (2- , 3-, 4-, 5-, or 7-) benzothienyl] methyl, [7-iodo- (2-, 3-, 4-,

5-, or 6-) benzothienyl] methyl, [2-chloro- (3-, 4-, 5-, 6-, or 7-) benzothienyl] methyl, [4,5-dichloro- (2-, 3- , 6-, or 7-) benzothienyl] methyl, [2,4,5-chloro- (3-, 6- or 7-)

benzothienyl] methyl, 2- [6-fluoro- (2-, 3-, 4-, 5-, or 7-) benzothienyl] ethyl, 1- [7-iodo- (2-, 3-, 4-, 5 -, or 6-) benzothienyl] ethyl, 3- [2-chloro- (3-, 4-, 5-, 6-, or 7-) benzothenyl] propyl, 4- [4,5-dichloro- ( 2-, 3-, 6-, or 7-) benzothienyl] butyl, 5- [2,4,5-trichloro- (3-, 6- or 7-) benzothienyl] pentyl, and 6- [5-chloro- (2-, 3-, 4-, 6-, or 7-) benzothienylhexyl.

Examples of lower alkynyl groups include straight and branched C 2-6 alkynyl groups such as ethinyl, 2-propynyl, 2-butynyl, 3-butynyl, 1-methyl-2-propynyl, 2-pentynyl, and 2-hexynyl.

Examples of lower alkenyl groups include straight and branched C 2-6 alkenyl groups containing one to three double bonds, such as vinyl, 1-propenyl, 1-methyl-1-propenyl, 2-methyl-1-propenyl, 2 -propenyl, 2-butenyl, 1-butenyl, 3-butenyl, 2-pentenyl, 1-pentenyl, 3-pentenyl, 4-pentenyl, 1,3-butadienyl, 1,3-pentadienyl, 2-penten-4-yl , 2-hexenyl, 1-hexenyl, 5-hexenyl, 3-hexenyl, 4-hexenyl, 3,3-dimethyl-1-propenyl, 2-ethyl-1-propenyl, 1,3,5-hexatrienyl, 1,3 hexadienyl, and 1,4-hexadienyl.

Examples of lower benzoalkyl imidazolyl groups include benzoimidazolylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as [(1-, 2-, 4-, or 5-) benzoimidazolyl] methyl , 2 - [(1-, 2-, 4-, or 5-) benzoimidazolyl] ethyl, 1 - [(1-, 2-, 4-, or 5-) benzoimidazolyl] ethyl, 3 - [(1 -, 2-, 4-, or 5-) benzoimidazolyl] propyl, 4 - [(1-, 2-, 4-, or 5-) benzoimidazolyl] butyl, 5 - [(1-, 2-, 4 -, or 5-) benzoimidazolyl] pentyl, 6 - [(1-, 2-, 4-, or 5-) benzoimidazolyl] hexyl, 1,1-dimethyl-2 - [(1-, 2-, 4-, or 5-) benzoimidazolyl] ethyl, and 2-methyl-3 - [(1-, 2-, 4-, or 5-) benzoimidazolyl] propyl.

Examples of pyridyl lower alkyl groups include pyridylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, such as [(2-, 3-, or 4-) pyridyl] methyl, 2- [(2-, 3-, or 4-) pyridyl] ethyl, 1 - [(2-, 3-, or 4-) pyridyl] ethyl, 3 - [(2-, 3-, or 4-) pyridyl] propyl, 4 - [(2-, 3-, or 4-) pyridyl] butyl, 1,1-dimethyl-2 - [(2-, 3-, or 4-) pyridyl] ethyl, 5 - [( 2-, 3-, or 4-) pyridyl] pentyl, 6 - [(2-, 3-, or 4-) pyridyl] hexyl, 1 - [(2-, 3-, or 4-) pyridyl] isopropyl, and

2-methyl-3 - [(2-, 3-, or 4-) pyridyl] propyl.

Examples of imidazolyl lower alkyl groups optionally substituted on the imidazole ring with one or more phenyl lower alkyl groups include:

imidazolylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the imidazole ring with one to three phenylalkyl groups described above wherein the alkyl moiety is a straight or branched C 1-6 alkyl group;

such as [(1-, 2-, 4-, or 5-) imidazolyl] methyl, 2 - [(1-, 2-, 4-, or 5-) imidazolyl] ethyl, 1 - [(1-, 2 -, 4-, or 5-) imidazolyl] ethyl, 3 - [(1-, 2-, 4-, or 5-) imidazolyl] propyl, 4 - [(1-, 2-, 4-, or 5-) imidazolyl] butyl, 1,1-dimethyl-2 - [(1-, 2-, 4-, or 5-) imidazolyl] ethyl, 5 - [(1-, 2-, 4-, or 5- ) imidazolyl] pentyl, 6 - [(1-, 2-, 4-, or 5-) imidazolyljhexyl, 1 - [(1-, 2-, 4-, or 5-) imidazolyljisopropyl, 2-methyl-3- [ (1-, 2-, 4-, or 5-) imidazolyl] propyl, [1-benzyl- (2-, 4-, or 5-) imidazolyl] methyl, [1- (2-phenylethyl) - (2-, 4 -, or 5-) imidazolyl] methyl, [1- (1-phenylethyl) - (2-, 4-, or 5-) imidazolyl] methyl, [1- (3-phenylpropyl) - (2-, 4 -, or 5-) imidazolyl] methyl, [1- (4-phenylbutyl) - (2-, 4-, or 5-) imidazolyl] methyl, [1- (5-phenylpentyl) - (2-, 4-, or 5 -) imidazolyl] methyl, [1- (6-phenylexyl) - (2-, 4-, or 5-) imidazolyl] methyl, 2- [2-benzyl- (1-, 4-, or 5-) imidazolyljetyl, 1- [4- (4-phenylethyl) - (1- or 2-) imidazolyljetyl, 3- [2- (2-phenylethyl) - (1-, 4-, or 5-) imidazolyl] methyl, 4- [1- (3- phenylpropyl) - (2- , 4-, or 5-) imidazolyl] butyl, 5- [1- (4-phenylbutyl) - (2-, 4-, or 5-) imidazolyl] butyl, 6- [1- (5-phenylpentyl) - (2-, 4 -, or 5-) imidazolyl] hexyl, [1,2-dibenzyl- (4- or 5-) imidazolyl] methyl, and (1,2,4-tribenzyl-5-imidazolyl) methyl.

Examples of lower alkylsulfonyl groups optionally substituted with one or more halogen atoms include straight and branched C1-6 alkylsulfonyl groups optionally substituted with one to three halogen atoms, such as, in addition to the lower alkylsulfonyl groups, trifluoromethylsulfonyl, trichloromethylsulfonyl, chloromethylsulfonyl, bromomethylsulfonyl, fluoromethylsulfonyl, iodomethylsulfonyl, difluoromethylsulfonyl, dibromomethylsulfonyl, 2-chloroethylsulfonyl, 2,2,2-trifluoroethylsulfonyl, chloropropylsulfonyl, 4,4-trichlorobutylsulfonyl, 4-fluorobutylsulfonyl, 5-chloropentylsulfonyl, 3-chloro-2-methylpropylsulfonyl, 5-bromohexylsulfonyl, and 5,6-dibromoexylsulfonyl described above.

Examples of alkoxycarbonyl groups optionally substituted by one or more halogen atoms include:

alkoxycarbonyl groups wherein the alkoxy moiety is a straight or branched alkoxy group, optionally substituted with one to three halogen atoms;

such as, in addition to the lower alkoxycarbonyl groups, i-heptyloxycarbonyl, n-octyloxycarbonyl, n-nonyloxycarbonyl, i-decyloxycarbonyl, 2-ethylhexyloxycarbonyl, trifluoromethoxycarbonyl, trichloromethoxycarbonyl, chloro-methoxycarbonylcarbomethoxycarbonylcarbonylcarbonyl, , dibromomethoxycarbonyl, 2-chloroethoxycarbonyl, 2-fluoroethoxycarbonyl, 2,2,2-trifluoroethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl, 3-chloropropoxycarbonyl, 2,3-dichloropropoxycarbonyl, 4,4,4-trichlorobutoxycarbonyl , 4-fluorobutoxycarbonyl, 4-chlorobutoxycarbonyl, 5-chloro-pentyloxycarbonyl, 3-chloro-2-methylpropoxycarbonyl, 5-bromoexyloxycarbonyl, 5,6-dibromoexyloxycarbonyl, 7,7,6-trichloroeptyloxycarbonyl, 8-bromooctyloxycarbonyl 9-trifluorononyloxycarbonyl; and 10,10,10-trichlorodecyloxycarbonyl described above.

Examples of pyridylcarbonyl groups optionally substituted on the pyridine ring with one or more members selected from the group consisting of pyrrolyl groups and halogen atoms include:

pyridylcarbonyl groups optionally substituted on the pyridine ring with one to three members selected from the group consisting of pyrrolyl groups and halogen atoms; such as (2-, 3-, or 4-) pyridylcarbonyl, 2-chloro- (3-, 4-, 5-, or 6-)

pyridylcarbonyl, 2,6-dichloro- (3-, 4-, or 5-) pyridylcarbonyl, 2- (1-pyrrolyl) - (3-, 4-, 5-, or 6-) pyridylcarbonyl, 2-bromo- ( 3-, 4-, 5-, or 6-) pyridylcarbonyl, 2,6-difluoro- (3-, 4-, or 5-) pyridylcarbonyl, 4- (1-pyrrolyl) - (2- or 3-) pyridylcarbonyl , 3-chloro- (2-, 4-, 5-, or 6-) pyridylcarbonyl, 2,5-dibromo- (3-, 4-, or 6-) pyridylcarbonyl, 2- (1-pyrrolyl) - 4-chloro- (3-, 5-, or 6-) pyridylcarbonyl, 2,4,6-trifluoro- (3- or 5-) pyridylcarbonyl, and 2,4-di (1-pyrrolyl) - (3-, 5-, or 6-) pyridylcarbonyl.

Examples of pyridine ring optionally substituted pyridyl groups with one or more members selected from the group consisting of lower alkyl groups and lower alkoxy groups include: optionally substituted pyridine ring pyridyl groups with

one to three members selected from the group consisting of the linear and branched C 1-6 alkyl groups described above and the linear and branched C 1-6 alkoxy groups described above;

such as (2-, 3-, or 4-) pyridyl, 2-methyl- (3-, 4-, 5-, or 6-) pyridyl, 3-methyl- (2-, 4-, 5-, or 6-) pyridyl, 2-methoxy- (3-, 4-, 5-, or 6-) pyridyl, 4-ethyl- (2- or 3-) pyridyl, 3-n-propyl- (2-, 4- , 5-, or 6-) pyridyl, 2-tert-butyl- (3-, 4-, 5-, or 6-) pyridyl, 2-n-pentyl- (3-, 4-, 5-, or 6 -) pyridyl, 3-n-hexyl- (2-, 4-, 5-, or 6-) pyridyl, 2,4-dimethyl- (3-, 5-, or 6-) pyridyl, 2,4,6 -trimethyl- (3- or 5-) pyridyl, 3-ethoxy- (2-, 4-, 5-, or 6-) pyridyl, 2-isopropoxy- (3-, 4-, 5-, or 6-) pyridyl, 2-n-butoxy (3-, 4-, 5-, or 6-) pyridyl, 4-n-pentyloxy (2- or 3-) pyridyl, 2-n-hexyloxy (3-, 4) -, 5-, or 6-) pyridyl, 2,3-dimethoxy- (4-, 5-, or 6-) pyridyl, 3-methyl- (2-, 4-, 5-, or 6-) pyridyl, 3,4,5-trimethoxy- (2- or 6-) pyridyl, and 2-methyl-3-methoxy- (4-, 5-, or 6-) pyridyl.

Examples of amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups:

include amino groups optionally substituted with one or two members selected from the group consisting of straight and branched C1-6 alkyl groups and straight and branched C1-6 alkanoyl groups;

such as amino, methylamino, ethylamino, n-propylamino, isopropylamino, n-butylamino, tert-butylamino, n-pentylamino, n-hexylamino, dimethylamino, diethylamino, di-n-propylamino, di-n-butylamino, di-n-pentylamino, di-n-hexylamino, N-methyl- / N-ethylamino, N-ethyl- / N-propylamino, N-methyl- / N-butylamino, N-methyl-A / -n-hexylamino, formylamino, acetylamino, propionylamino, butyrylamino, isobutyrylamino, pentanoylamino, tert-butylcarbonylamino, hexanoylamino, Î ± / V-diacetylamino, Î ± -acetyl - β / - propionylamino, Î ± - methyl-V-acetylamino, and N-ethyl-propionylamino. Examples of optionally substituted pyrrolidinyl groups on the

Pyrrolidine ring with one or more oxo groups include pyrrolidinyl groups optionally substituted with one or two oxo groups, such as (1-, 2-, or 3-) pyrrolidinyl, 2-oxo- (1-, 3-, 4- , or 5-) pyrrolidinyl, and 2,5-dioxo- (1- or 3-) pyrrolidinyl.

Examples of optionally substituted piperidinyl groups on the

Piperidine ring having one or more lower alkyl groups include optionally substituted piperidinyl groups on the piperidine ring having one to three straight and / or branched C1-6 alkyl groups, such as (1-, 2-, 3-, or 4-) piperidinyl, 1-methyl- (2-, 3-, or 4-) piperidinyl, 1-ethyl- (2-, 3-, or 4-) piperidinyl, 1-n-propyl- (2-, 3-, or 4-) piperidinyl, 1-isopropyl- (2-, 3-, or 4-) piperidinyl, 1- n -butyl- (2-,

3-, or 4-) piperidinyl, 1-n-pentyl- (2-, 3-, or 4-) piperidinyl, 1-n-hexyl- (2-, 3-, or

4-) piperidinyl, 1,2-dimethyl- (3-, 4-, 5-, or 6-) piperidinyl, 1,2,3-trimethyl- (4-, 5-, or 6-) piperidinyl, 2- n-propyl- (1-, 3-, 4-, 5- or 6-) piperidinyl, 3-ethyl- (1-, 2-, 4-, 5-, or 6-) piperidinyl, and 2-methyl- 4-Isopropyl- (1-, 3-, 5-, or 6-) piperidinyl.

Examples of carbamoyl groups optionally substituted with one or more lower alkyl groups include carbamoyl groups optionally substituted with one or two straight and / or branched C1-6 alkyl groups, such as carbamoyl, methylcarbamoyl, ethylcarbamoyl, n-propylcarbamoyl, isopropylcarbamoyl, n-butylcarbamoyl , tert-butylcarbamoyl, n-pentylcarbamoyl, n-hexylcarbamoyl, dimethylcarbamoyl, diethylcarbamoyl, di-n-propyl carbamoyl, di-n-butylcarbamoyl, di-n-hexylcarbamoyl, N-ethylcarbamoyl, N-ethyl- N-propylcarbamoyl, N-methyl- N-N-butylcarbamoyl and N-methyl- N-hexylcarbamoyl.

Examples of phenyl groups optionally substituted on the ring with one or more members selected from the group consisting of halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; a phenoxy group; lower alkoxy groups optionally substituted with one or more halogen atoms; lower alkylthio groups; lower alkylsulfonyl groups; amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups; pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups; piperidinyl groups optionally substituted on the piperidine ring with one or more lower alkyl groups; lower alkenyl groups; an aminosulfonyl group; a hydroxy group; carbamoyl groups optionally substituted by one or more lower alkyl groups; phenyl lower alkoxy groups; and a cyan group include:

optionally substituted phenyl groups on the phenyl ring having one to three members selected from the group consisting of the halogen atoms described above; the above described straight and branched C 1-6 alkyl groups optionally substituted with one to three halogen atoms; a phenoxy group; the linear and branched C1-6 alkoxy groups described above optionally substituted with one to three halogen atoms; the linear and branched C 1-6 alkylthio groups described above; the linear and branched C1-6 alkylsulfonyl groups described above; the amino groups described above optionally substituted with one or two members selected from the group consisting of straight and branched C1-6 alkyl groups and straight and branched C1-6 alkanoyl groups; optionally substituted pyrrolidinyl groups described above on the pyrrolidine ring with one or two oxo groups; the optionally substituted piperidinyl groups described above on the piperidine ring having one to three straight and / or branched C1-6 alkyl groups; the linear and branched C 2-6 alkenyl groups described above containing one to three double bonds; an aminosulfonyl group; a hydroxy group; optionally substituted carbamoyl groups described above with one or two straight and / or branched C1-6 alkyl groups; phenylalkoxy groups described above wherein the alkoxy moiety is a straight and branched C1-6 alkoxy group; and a cyan group;

such as phenyl, 4-phenoxyphenyl, 3-phenoxyphenyl, 2-phenoxyphenyl, 4-isopropylphenyl, 3-isopropylphenyl, 2-isopropylphenyl, 4-tert-butylphenyl, 4-methylphenyl, 3-methylphenyl, 2-methylphenyl, 2, 3-dimethylphenyl, 2,4-dimethylphenyl, 3,5-dimethylphenyl, 2,4,6-trimethylphenyl, 4-methyl-3-methoxyphenyl, 4-trifluoromethylphenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 4-methyl-3- chlorophenyl, 4-chlorophenyl, 3-chlorophenyl, 2-chlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-bromophenyl, 3,4-dichlorophenyl, 3,5-dichlorophenyl, 3,4,5-trichlorophenyl, 2,4,6-trifluorophenyl, 3,5-difluorophenyl, 3-chloro-4-fluorophenyl, 2-chloro-5-fluorophenyl, 3-fluoro-4-methoxyphenyl, 3-chloro-4-methoxyphenyl, 3-chloro- 4-hydroxyphenyl, 4-methoxyphenyl, 3-methoxyphenyl, 2-methoxyphenyl, 2,4-dimethoxyphenyl, 3,4-dimethoxyphenyl, 2,4,6-trimethoxyphenyl, 2-methoxy-5-chlorophenyl, 2- methoxy-5-acetylamino-phenyl, 2-chloro-5-acetylaminophenyl, 4-ethoxyphenyl, 4-trifluoromethoxyphenyl, 3-trifluoromethoxyphenyl, 2-trifl uoromethoxyphenyl, 3-methoxy-5-trifluoromethylphenyl, 4-methylthiophenyl, 3-methylthiophenyl, 2-methylthiophenyl, 2- (1-methyl-1-vinyl) phenyl, 4-vinylphenyl, 3-dimethylaminophenyl, 4-methylaminophenyl, 2- ( N -methyl- (N-acetylamino) phenyl, 3-acetylaminophenyl, 4-propionylaminophenyl, 4-acetylaminophenyl, 2-acetylaminophenyl, 4-aminosulfonylphenyl, 3-aminosulfonylphenyl, 2-aminosulfonylphenyl, 4-methylthiophenyl, 3-methylthiophenyl 2-methylthiophenyl, 4-methylsulfonyl phenyl, 3-methylsulfonylphenyl, 2-methylsulfonylphenyl, 4-methylcarbamoylphenyl, 3-carbamoylphenyl, 2-ethylcarbamoylphenyl, 2-benzyloxyphenyl, 3-benzyloxyphenyl, 2-benzyloxyphenyl, 2-benzyloxyphenyl phenylphenyl, 4-phenylphenyl, 2-cyanophenyl, 3-cyano-phenyl, 4-cyanophenyl, 4- [2-oxo- (1-, 3-, 4-, or 5-) pyrrolidinyl] phenyl, 3- [2, 5-dioxo- (1- or 3-) pyrrolidinyl] phenyl, 4- [4-methyl- (1-, 2-, or 3-) piperazinyl] phenyl, 3- [4-ethyl- (1-, 2-, or 3-) piperazinyl] phenyl, and 2- [4-isopropyl- (1-, 2-, or 3-) piperazinyl] phenyl.

Examples of optionally substituted cycloalkyl ring alkyl groups with one or more lower alkyl groups include C 3-8 alkyl groups optionally substituted on the cycloalkyl ring having one to three straight and / or branched C1-6 alkyl groups, such as, in addition to the groups cycloalkyl, 1-methylcyclopropyl, 1-methylcyclopentyl, 1-methylcyclohexyl, 2-methylcyclohexyl, 1-methylcyclobutyl, 1-ethylcyclooctyl, 1-n-propylcycloeptyl, 1,2-dimethylcyclohexyl, 1,4,5-trimethylcycloethyl, n-butylcyclopropyl, 1-n-pentylcyclopentyl, and 1-r'hexylcyclopexyl described above. Examples of amino groups optionally substituted with one

or more members selected from the group consisting of a phenyl group and lower alkyl groups include:

amino groups optionally substituted with one or two members selected from the group consisting of a phenyl group and straight and branched C 1-6 alkyl groups;

such as amino, methylamino, ethylamino, i-propylamino, isopropylamino, n-butylamino, tert-butylamino, π-pentylamino, n-hexylamino, dimethylamino, diethylamino, di-n-propylamino, di-n-butylamino , di-n-pentylamino, di-n-hexylamino, Î ± -methyl- β-ethylamino, Î ± -ethyl-Î ± -n-propylamino, Î ± -methyl-Î ± -n-butylamino, / N-methyl- / N-hexylamino, phenylamino, N / N-diphenylamino, N-methyl-N / phenylamino, N-ethyl- N-phenylamino, and N-N-propyl / N- phenylamino.

Examples of benzoyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; a phenoxy group; a phenyl group; lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups; lower alkanoyl groups; a nitro group; a cyan group; amino groups optionally substituted with one or more members selected from the group consisting of a phenyl group and lower alkyl groups; pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups; pyrrolyl groups; pyrazolyl groups; 1,2,4-triazolyl groups; and imidazolyl groups include: optionally substituted benzoyl groups on the phenyl ring with

one to three members selected from the group consisting of halogen atoms; a phenoxy group; a phenyl group; the linear and branched C1-6 alkyl groups described above optionally substituted with one to three halogen atoms; the linear and branched C1-6 alkoxy groups described above; the linear and branched C1-6 alkanoyl groups described above; a nitro group; a cyan group; the amino groups described above optionally substituted with one or two members selected from the group consisting of a phenyl group and straight and branched C1-6 alkyl groups; the above-described pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or two oxo groups; pyrrolyl groups; pyrazolyl groups; 1,2,4-triazolyl groups; and imidazolyl groups;

such as benzoyl, 4-methoxybenzoyl, 3-methoxybenzoyl, 2-methoxybenzoyl, 2,4-dimethoxybenzoyl, 3,4,5-trimethoxybenzoyl, 2-methoxy-5-chloro-benzoyl, 4-phenoxybenzoyl, 2-phenoxybenzoyl, 3-phenoxybenzoyl, 4-chlorobenzoyl, 3-chlorobenzoyl, 2-chlorobenzoyl, 2,6-dichlorobenzoyl, 2-chloro-4-fluorobenzoyl, 2,4,6-trifluorobenzoyl, 4-bromobenzoyl, 3-fluorobenzoyl, 4-trifluoromethylbenzoyl, 3-trifluoromethylbenzoyl, 2-trifluoromethylbenzoyl, 3-fluoro-2-methylbenzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 3,4-dimethylbenzoyl, 2,4,5-trimethylbenzoyl, 2- phenylbenzoyl, 3-phenylbenzoyl, 4-phenylbenzoyl, 4-nitrobenzoyl, 3-nitrobenzoyl, 2-nitrobenzoyl, 2-dimethylaminobenzoyl, 3-methylaminobenzoyl, 4- (β-methylanilino) benzoyl, 2-anilino benzoyl , 3-cyanobenzoyl, 4-cyanobenzoyl, 2-cyanobenzoyl, 4-acetylbenzoyl, 2-propionylbenzoyl, 3-butyrylbenzoyl, 4 - [(1-, 2-, or 3-) pyrrolyl] benzoyl, 4 - [(1 -, 3-, 4-, or 5-) pyrazole yl] benzoyl, 4 - [(1-, 3- or 5-) 1,2,4-triazolyl] benzoyl, 4 - [(1-, 2-, 4-, or 5-) imidazolyl] benzoyl, and 4 - [2-oxo- (1-, 3-, 4-, or 5-) pyrrolidinyl] benzoyl.

Examples of lower alkylenedioxy groups include straight or branched C1-4 alkylene groups, such as methylenedioxy, ethylenedioxy, trimethylenedioxy, and tetramethylenedioxy.

Examples of phenyl ring substituted benzoyl groups with one or more lower alkylenedioxy groups include:

phenyl ring substituted benzoyl groups having one or more of the linear or branched C 1-4 alkylenedioxy groups described above;

such as 3,4-methylenedioxybenzoyl, 2,3-ethylenedioxybenzoyl, 3,4-trimethylenedioxybenzoyl, and 2,3-tetramethylenedioxybenzoyl.

Examples of cycloalkylcarbonyl groups include cycloalkylcarbonyl groups wherein the cycloalkyl moiety is a C3.8 cycloalkyl group, such as cyclopropylcarbonyl, cyclobutylcarbonyl, cyclopentylcarbonyl, cyclohexylcarbonyl, cycloeptylcarbonyl, and cyclooctylcarbonyl.

Examples of furylcarbonyl groups include (2- or 3-) furylcarbonyl.

Examples of naphthylcarbonyl groups include (1- or 2-) naphthylcarbonyl

Bonila.

Examples of phenoxycarbonyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxy groups, lower alkyl groups, halogen atoms, and a nitro group include:

Phenoxycarbonyl groups optionally substituted on the phenyl ring with one to three members selected from the group consisting of the linear and branched C1-6 alkoxy groups described above, the linear and branched C1-6 alkyl groups described above, halogen atoms, and a nitro group;

Such as phenoxycarbonyl, 4-chlorophenoxycarbonyl, 3-chlorophenoxycarbonyl, 2-chlorophenoxycarbonyl, 3,4-dichlorophenoxycarbonyl, 2,4,6-trichlorophenoxycarbonyl, 4-fluorophenoxycarbonyl, 3-fluorophenoxycarbonyl, 2-fluorophenoxycarbonyl, 2, 4-difluorophenoxycarbonyl, 3,4,5-trifluorophenoxycarbonyl, 4-bromophenoxycarbonyl, 2-chloro-4-methoxyphenoxycarbonyl, 3-fluoro-5-methylphenoxycarbonyl, 4-methoxyphenoxycarbonyl, 3-methoxyphenoxycarbonyl, 3-methoxyphenyl 4-dimethoxyphenoxycarbonyl, 2,4,5-trimethoxyphenoxycarbonyl, 4-methylphenoxycarbonyl, 3-methylphenoxycarbonyl, 2-methylphenoxycarbonyl, 2,5-dimethylphenoxycarbonyl, 2,3,4-trimethylphenoxycarbonyl, 4-nitrophenoxycarbonyl, 3-nitrophenoxycarbonyl, 2-nitrophenoxycarbonyl, 2,4-dinitrophenoxycarbonyl, and 2,4,6-trinitrophenoxycarbonyl.

Examples of phenyl lower alkoxycarbonyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and one nitro group include:

phenylalkoxycarbonyl groups wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group, optionally substituted on the phenyl ring with one to three members selected from the group consisting of halogen atoms and a nitro group;

such as benzyloxycarbonyl, 2-phenylethoxycarbonyl, 1-phenylethoxycarbonyl, 3-phenylpropoxycarbonyl, 4-phenylbutoxycarbonyl, 5-phenylpentyloxycarbonyl, 6-phenylhexyloxycarbonyl, 1,1-dimethyl-2-phenylethoxycarbonyl, 2-methyloxycarbonyl 4-chlorobenzyloxycarbonyl, 3-chlorobenzyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 3,4-dichlorobenzyloxycarbonyl, 2,4,6-trichlorobenzyloxycarbonyl, 4-fluorobenzyloxycarbonyl, 3-fluorobenzyloxycarbonyl, 2-fluoro-benzyloxycarbonyl, 2,4-difoxyl 4,5-Trifluorobenzyloxycarbonyl, 4-bromobenzyloxycarbonyl, 4-nitrobenzyloxycarbonyl, 3-nitrobenzyloxycarbonyl, 2-nitrobenzyloxycarbonyl, 2,4-dinitrobenzyloxycarbonyl, 2,4,6-tri-nitrobenzyloxycarbonyl, and 2-nitro-4-benzyloxycarbonyl .

Examples of piperidinyl groups optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl group; lower alkanoyl groups; optionally substituted benzoyl groups on the phenyl ring having one or more halogen atoms; and optionally substituted phenyl groups on the phenyl ring with one or more halogen atoms include:

optionally substituted piperidinyl groups on the one to three membered piperidine ring selected from the group consisting of the linear and branched C1-6 alkyl groups described above; C1-6 alkanoyl or branched groups described above; in the optionally substituted benzoyl groups described above described above on the phenyl ring having one to three halogen atoms; and the above described phenyl groups optionally substituted on the phenyl ring having one to three halogen atoms;

such as (1-, 2-, 3-, or 4-) piperidinyl, 1-methyl- (2-, 3-, or 4-) piperidinyl, 1-acetyl- (2-, 3-, or 4 -) piperidinyl, 1-benzoyl- (2-, 3-, or 4-) piperidinyl, 1- (4-chlorobenzoyl) - (2-, 3-, or 4-) piperidinyl, 1- (3-bromobenzoyl) ) - (2-, 3-, or 4-) piperidinyl, 1-benzoyl- (2-, 3-, or 4-) piperidinyl, 1- (4-fluorobenzoyl) - (2-,

3-, or 4-) piperidinyl, 1- (2,4-dichloro benzoyl) - (2-, 3-, or 4-) piperidinyl, 1- (2,4,6-trifluorobenzoyl) - (2-, 3 -, or 4-) piperidinyl, 2- (3-chlorobenzoyl) - (1-, 3-, or

4-) piperidinyl, 3- (2-chlorobenzoyl) - (1-, 2-, or 4-) piperidinyl, 4- (2,3-dibrobenzoyl) - (1-, 2-, or 3-) piperidinyl 1,2-dibenzoyl- (3- or 4-) piperidinyl,

1,2,4-tribenzoyl-3-piperidinyl, 1,4-dimethyl- (2-, 3-, 5-, or 6-) piperidinyl, 1,2,4-trimethyl- (3-, 5-, or 6-) piperidinyl, 1-benzoyl-2-methyl- (3-, 4-, 5-, or 6-) piperidinyl, 1-phenyl-2-methyl- (3-, 4-, 5-, or 6-) piperidinyl, 1-acetyl-3-methyl- (2-, 4-, 5-, or 6-) piperidinyl, 1-phenyl- (2-, 3-, or 4-) piperidinyl, 1- (4 -chlorophenyl) - (2-, 3-, or 4-) piperidinyl, 1- (3-bromophenyl) - (2-, 3-, or 4-) piperidinyl, 1- (4-iodophenyl) - (2-, 3-, or 4-) piperidinyl, 1- (4-fluorophenyl) - (2-, 3-, or 4-) piperidinyl, 1- (2,4-dichlorophenyl) - (2-, 3-, or 4- ) piperidinyl, 1- (2,4,6-trifluorophenyl) - (2-, 3-, or 4-) piperidinyl, 2- (3-chlorophenyl) - (1-, 3-, 4-, 5-, or 6-) piperidinyl, 3- (2-chlorophenyl) - (1-, 2-, 4-, 5-, or 6-) piperidinyl, 4- (2,3-dibromophenyl) - (1-, 2-, or 3-) piperidinyl, 1,2-diphenyl- (3-, 4-, 5- or 6-) piperidinyl, and 1,2,4-triphenyl- (3-, 5-, or 6-) piperidinyl dinila.

Examples of lower alkyl tetrahydropyranyl groups include tetrahydropyranylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as [(2-, 3-, or 4-) tetrahydropyranyl] methyl, 2- [ (2-, 3-, or 4-) tetrahydropyranyl] ethyl, 1 - [(2-, 3-, or 4-) tetrahydropyranyl] ethyl, 3 - [(2-, 3-, or 4-) tetrahydropyranyl] propyl , 4 - [(2-, 3-, or 4-) tetrahydropyranyl] butyl, 1,1-dimethyl-2 - [(2-, 3-, or 4-) tetrahydropyranyl] ethyl, 5 - [(2-, 3-, or 4-) tetrahydropyranyl] pentyl, 6 - [(2-, 3-, or 4-) tetrahydropyranyl] hexyl, 1 - [(2-, 3- or 4-) tetrahydropyranyl] isopropyl, and 2 -methyl-3 - [(2-, 3-, or 4-) tetrahydropyranyl] propyl.

Examples of phenyl lower alkyl groups optionally substituted on the alkyl group with one or more lower alkoxycarbonyl groups; and optionally also substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms, lower alkyl groups optionally substituted with one or more halogen atoms, lower alkoxy groups optionally substituted with one or more halogen atoms, and a hydroxy group include:

Mono- and di-phenylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the alkyl group with one or more lower alkoxycarbonyl groups wherein the alkoxy moiety is a C1-6 group straight or branched alkoxy; and optionally also substituted on the phenyl group with one to three members selected from the group consisting of halogen atoms, on the linear and branched C1-6 alkyl groups described above optionally substituted on one to three halogen atoms, on the groups Linear and branched C1-6 alkoxy described above optionally substituted with one to three halogen atoms, and one hydroxy group;

such as benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenylhexyl, 2-methyl-3-phenylpropyl, 1, 1-Dimethyl-2-phenylethyl, 1,1-dimethyl-1-phenylmethyl, 1,1-diphenylmethyl, 2,2-diphenylethyl, 3,3-diphenylpropyl, 1,2-diphenylethyl, 4-chlorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 3-fluorobenzyl, 4-fluorobenzyl, 3-bromobenzyl, 2,3-dichlorobenzyl, 2,6-dichlorobenzyl, 2,4,6-trifluorobenzyl, 2- (4-chlorophenyl) ethyl, 2- ( 2-fluorophenyl) ethyl, 2- (3-fluorophenyl) ethyl, 3-trifluoromethylbenzyl, 4-trifluoromethylbenzyl, 2-methylbenzyl, 3-methylbenzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 2,4-dimethylbenzyl, 2 4,6-trimethylbenzyl, 2-trifluoromethoxybenzyl, 3-trifluoromethoxybenzyl, 4-trifluoromethoxybenzyl, 2-methoxybenzyl, 3-methoxybenzyl, 4-methoxybenzyl, 4-ethoxybenzyl, 2- (3-methoxyphenyl) ethyl, 3,4- dimethoxybenzyl, 3,4,5-trimethoxybenzyl, 4-hydroxybenzyl, 3-hydroxybenzyl, 2-hydroxybenzyl, 2,4-dihydroxybenzyl, 3,4,5-t hydroxybenzyl, 2-methoxy-4-chlorobenzyl, 3-methyl-5-fluorobenzyl, 2- (4-hydroxyphenyl) -1-methoxycarbonylethyl, and 2- (4-chlorophenyl) -1-ethoxycarbonylethyl.

Examples of lower alkylenodioxy substituted phenyl lower alkyl groups include:

alkylenedioxy substituted phenylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group substituted on the phenyl ring with one or more of the above described linear or branched C 1-4 alkylenedioxy groups;

such as 3,4-methylenedioxybenzyl, 3,4-trimethylenedioxybenzyl, 2- (2,3-ethylenedioxyphenyl) ethyl, 1- (3,4-trimethylenedioxyphenyl) ethyl, 3- (2,3-tetramethylenedioxyphenyl) propyl, 4 - (3,4-methylenedioxyphenyl) butyl, 5- (2,3-ethylenedioxyphenyl) pentyl, 6- (3,4-trimethylenedioxyphenyl) hexyl, 1,1-dimethyl-2- (2,3-methylenedioxyphenyl) ethyl , and 2-methyl-3- (3,4-ethylenedioxyphenyl) propyl.

Examples of furyl lower alkyl groups include furylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, such as [(2- or 3-) furylmethyl, 2 - [(2- or 3-) furyl ] ethyl, 1 - [(2- or 3-) furyl] ethyl, 3 - [(2- or 3-) furyl] propyl, 4 - [(2- or 3-) furyl] butyl, 5 - [(2 - or 3-) furyl] pentyl, 6 - [(2- or 3-) furyl] hexyl, 1,1-dimethyl-2 - [(2- or 3-) furyl] ethyl, and 2-methyl-3- [(2- or 3-) furyl] propyl.

Examples of lower alkylcarbamoyl groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and one phenyl group, each phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups, include:

Carbamoylalkyl groups wherein the alkyl moiety is a linear or branched C1-6 alkyl group, optionally substituted with one or two members selected from the group consisting of the linear and branched C1-6 alkyl groups described above and the above described optionally substituted phenyl groups phenyl ring having one to three straight and / or branched C1-6 alkyl groups;

such as carbamoylmethyl, 2-carbamoylethyl, 1-carbamoylethyl, 3-

carbamoylpropyl, 4-carbamoylbutyl, 5-carbamoylpentyl, 6-carbamoylhexyl, 1,1-dimethyl-2-carbamoylethyl, 2-methyl-3-carbamoylpropyl, 2- (N-methyl-A / -phenylcarbamoyl) ethyl, A / - (4-methylphenyl) carbamoylmethyl, 2 - [/ V-methyl-A / - (3-methylphenyl) carbamoyl] ethyl, / V- (2-methylphenyl) carbamoylmethyl, 2 - [/ V-ethyl- / V- (3,4-dimethylphenyl) carbamoyl] ethyl, N / - (2,4,6-trimethylphenyl) carbamoylmethyl, N / N-dimethylcarbamoyl methyl, N, N-diphenylcarbamoylmethyl, / V-methyl N -ethylcarbamoylmethyl, N-methylcarbamoylmethyl, and 2- (N-methylcarbamoyl) ethyl.

Examples of imidazolyl lower alkyl groups optionally substituted on the lower alkyl group with one or more members selected from the group consisting of a carbamoyl group and lower alkoxycarbonyl groups include:

Imidazolylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the lower alkyl group with one or more members selected from the group consisting of a carbamoyl group and alkoxycarbonyl groups wherein the alkoxy moiety is a group. - po linear or branched C1-6 alkoxy;

Such as in addition to the above described lower alkyl imidazolyl, 1-carbamoyl-2 - [(1-, 2-, 4-, or 5-) imidazolyl] ethyl, 1-methoxycarbonyl-2 - [(1-, 2- , 4-, or 5-) imidazolyljetyl, 1-carbamoyl-1 - [(1-, 2-, 4-, or 5-) imidazolyl] methyl, 1-ethoxycarbonyl-1 - [(1-, 2- , 4-, or 5-) imidazolyl] methyl, 1-carbamoyl-3 - [(1-, 2-, 4-, or 5-) imidazolyl] propyl, 1-n-propoxycarbonyl-4 - [(1-, 2-, 4-, or 5-) imidazolyl] butyl, 1-carbamoyl-5 - [(1-, 2-, 4-, or 5-) imidazolyl] pentyl, and 1-tert-butoxycarbonyl-6 - [( 1-, 2-, 4-, or 5-) imidazolyl] hexyl.

Examples of optionally substituted amino-substituted lower alkyl groups in each amino group with one or more lower alkyl groups include:

Amino substituted linear or branched C 1-6 alkyl groups optionally substituted on the amino group with one or two linear and / or branched C 1-6 alkyl groups;

such as aminomethyl, 2-aminoethyl, 1-aminoethyl, 3-aminopropyl, 4-aminobutyl, 5-aminopentyl, 6-aminoexyl, 1,1-dimethyl-2-aminoethyl, 2-methyl-3-aminopropyl, methylaminomethyl, 2-ethylaminoethyl, 3- [1-propylaminopropyl, 3-isopropylaminopropyl, 4-n-butylaminobutyl, 5-7-pentylaminopentyl, 6-n-hexylaminoexyl, dimethylaminoethyl, 2-diisopropylaminopropyl, 3-diisopropylaminopropyl, (A (-ethyl- (N-propylamino) methyl, and 2- (N-methyl- (N-hexylamino) methyl).

Examples of 2,3,4,5-tetrahydrofuryl groups optionally substituted on ring 2,3,4,5-tetrahydrofuran with one or more oxo groups include: 2,3,4,5-tetrahydrofuryl groups optionally substituted on ring 2 3,4,5-tetrahydrofuran with one or two oxo groups;

such as (2- or 3-) 2,3,4,5-tetrahydrofuryl, 2-oxo- (3-, 4-, or 5-) 2,3,4,5-tetrahydrofuryl, 3-oxo- (2 -, 4-, or 5-) 2,3,4,5-tetrahydrofuryl, and 2,5-dioxo- (3- or 4-) 2,3,4,5-tetrahydrofuryl.

Examples of pyrrolidinyl lower alkyl groups optionally substituted on the pyrrolidine ring with one or more lower alkyl groups include:

Pyrrolidinylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the pyrrolidine ring with one to three to the above described straight and / or branched C 1-6 alkyl groups;

such as [(1-, 2-, or 3-) pyrrolidinyl] methyl, 2 - [(1-, 2-, or 3-) pyrrolidinyl] ethyl, 1 - [(1-, 2-, or 3 -) pyrrolidinyl] ethyl, 3 - [(1-, 2-, or 3-) pyrrolidinyl] propyl,

4 - [(1-, 2-, or 3-) pyrrolidinyl] butyl, 5 - [(1-, 2-, or 3-) pyrrolidinyl] pentyl, 6 - [(1-, 2-, or 3-) pyrrolidinyl] hexyl, 1,1-dimethyl-2 - [(1-, 2-, or 3-) pyrrolidinyl] ethyl, 2-methyl-3 - [(1-, 2-, or 3-) pyrrolidinyl] propyl, 1-ethyl [(2- or 3-) pyrrolidinyl] methyl, 1-ethyl - [(2- or 3-) pyrrolidinyl] methyl, 2-methyl - [(1-, 3-, 4-, or 5-) pyrrolidinyl] methyl , 3-n-propyl - [(1-, 2-, 4-, or 5-) pyrrolidinyl] methyl, 1-n-butyl - [(2- or 3-) pyrrolidinyl] methyl, 2-n-pentyl [(1-, 3-, 4-, or 5-) pyrrolidinyl] methyl, 1- [hexyl - [(2- or 3-) pyrrolidinyl] methyl, 1,2-dimethyl - [(3-, 4-, or 5-) pyrrolidinyl] methyl, and 1,2,3-trimethyl - [(4- or

5-) pyrrolidinyl] methyl.

Examples of lower alkanoyl phenoxy groups include phenoxy alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group such as 2-phenoxyacetyl, 3-phenoxypropionyl, 2-phenoxypropionyl, 4-phenoxybutyryl, 5-phenoxypentanoyl, 6-phenoxyhexanoyl, 2,2-dimethyl-3-phenoxypropionyl, and 2-methyl-3-phenoxypropionyl.

Examples of lower alkyl morpholino groups include morpholinoalkyl groups wherein the alkyl moiety is a straight or branched C--β alkyl group such as [(2-, 3-, or 4-) morpholinomethyl, 2 - [(2-, 3-, or 4-) morpholinojetyl, 1 - [(2-, 3-, or 4-) morpholino] ethyl, 3 - [(2-, 3-, or 4-) morpholino] propyl, 4- [ (2-, 3-, or 4-) morpholino] butyl, 5 - [(2-, 3-, or 4-) morpholino] pentyl, 6 - [(2-, 3-, or 4-) morpholino] hexyl 1,1-dimethyl-2 - [(2-, 3-, or 4-) morpholino] ethyl, and 2-methyl-3 - [(2-, 3-, or 4-) morpholino] propyl.

Examples of lower pyridyl alkanoyl groups include pyridyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, such as 2 - [(2-, 3-, or 4-) pyridyl] acetyl, 3- [(2-, 3-, or 4-) pyridyl] propionyl, 2 - [(2-, 3-, or 4-) pyridyl] propionyl, 4 - [(2-, 3-, or 4-) pyridyl] butyryl, 5 - [(2-, 3-, or 4-) pyridyl] pentanoyl, 6 - [(2-, 3-, or 4-) pyridyl] hexanoyl, 2,2-dimethyl-3 - [(2- , 3-, or 4-) pyridyl] propionyl, and 2-methyl-3 - [(2-, 3-, or 4-) pyridyl] propionyl.

Examples of thienylcarbonyl groups include 2-thienylcarbonyl and 3-thienylcarbonyl.

Examples of thienyl lower alkanoyl groups include tyranyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, such as 2 - [(2- or 3-) thienyl] acetyl, 3 - [(2- or 3-) thienyl] propionyl, 2 - [(2- or 3-) thienyl] propionyl, 4 - [(2- or 3-) thienyl] butyryl, 5 - [(2- or 3-) thienyl] pentanoyl, 6 - [(2- or 3-) thienyl] hexanoyl, 2,2-dimethyl-3 - [(2- or 3-) thienyl] propionyl, and 2-methyl-3 - [(2- or 3-) thienyl] propionyl.

Examples of lower cycloalkyl alkanoyl groups include C 3-8 cycloalkyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group such as 2-cyclopropylacetyl, cyclohexylacetyl, 3-cyclopropylpropionyl, 2-cyclobutylpropionyl, 2- cyclopentylacetyl, 3-cyclopentylpropionyl, 4-cyclohexylbutyryl, 5-cycloheptylpentanoyl, 6-cyclooctylhexanoyl, 2,2-dimethyl-3-cyclohexylpropionyl, and 2-methyl-3-cyclopropylpropionyl.

Examples of isoxazolylcarbonyl groups optionally substituted on the isoxazole ring with one or more lower alkyl groups include isoxazoylcarbonyl groups optionally substituted on the isoxazole ring with one or two straight and / or branched C1-6 alkyl groups, such as (3-, 4-, or 5-) isoxazolylcarbonyl, [3,5-dimethyl-4-isoxazolyl] carbonyl, [3-ethyl- (4- or 5-) isoxazolyl] carbonyl, [4-n-propyl- (3- or 5-) isoxazolyl] carbonyl, [5 - butyl- (3- or 4-) isoxazolyl] carbonyl, [3-n-pentyl- (4- or 5-) isoxazolyl] carbonyl, and [4-r ? -hexyl- (3- or 5-) isoxazolyl] carbonyl.

Examples of pyrazylcarbonyl groups include 2-pyrazylcarbonyl.

Examples of optionally substituted piperidinylcarbonyl groups on the piperidine ring with one or more members selected from the group consisting of a benzoyl group and lower alkanoyl groups include:

Piperidinylcarbonyl groups optionally substituted on the one to three membered piperidine ring selected from the group consisting of a benzoyl group and the linear or branched C 1-6 alkanoyl groups described above;

such as (1-, 2-, 3-, or 4-) piperidinylcarbonyl, [1-acetyl- (2-, 3-, or 4-) piperidinylcarbonyl, [1-benzoyl- (2-, 3-, or 4 -) piperidinylcarbonyl, [2-propionyl- (1-, 3-, 5-, or 6-) piperidinylcarbonyl, [3-butyryl- (1-, 2-, 5-, or 6-) piperidinyl] carbonyl, [4-pentanoyl- (1-, 2-, or 3-) piperidinylcarbonyl, [1-hexanoyl- (2-, 3-, or 4-) piperidinyl] carbonyl, [1-acetyl-4-benzoyl- (2- , 3-, 5-, or 6-) piperidinylcarbonyl, and [1,2,4-triacetyl- (3-, 5-, or 6-) piperidinylcarbonyl.

Examples of chromanylcarbonyl groups include 2-chromanylcarbonyl, 3-chromanylcarbonyl, 4-chromanylcarbonyl, 5-chromanylcarbonyl, 6-chromanylcarbonyl, 7-chromanylcarbonyl, and 8-chromanylcarbonyl.

Examples of lower isoindolinyl alkanoyl groups optionally substituted on the isoindoline ring with one or more oxo groups include:

Isoindolinyl lower alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, optionally substituted on the isoindoline ring with one or two oxo groups;

such as 2 - [(1-, 2-, 4-, or 5-) isoindolinyl] acetyl, 3 - [(1-, 2-, 4-, or 5-) isoindolinyl] propionyl, 2 - [(1- , 2-, 4-, or 5-) isoindolinyl] propionyl, 4 - [(1-, 2-, 4-, or 5-) isoindolinyl] butyryl, 5 - [(1-, 2-, 4-, or 5-) isoindolinyl] pentanoyl, 6 - [(1-, 2-, 4-, or 5-) isoindolinyl] hexanoyl, 2,2-dimethyl-3 - [(1-, 2-, 4-, or 5- ) isoindolinyl] propionyl, 2-methyl-3 - [(1-, 2-, 4-, or 5-) isoindolinyl] propionyl, [1,3-dioxo-2- (2-, 4-, or 5 -) isoindolinyl] acetyl, and [1-oxo-2- (2-, 3-, 4-, 5-, 6-, or 7-) isoindolinyl] acetyl.

Examples of thiazolidinyl lower alkanoyl groups optionally substituted on the thiazolidine ring with one or more members selected from the group consisting of an oxo group and a thioxo group include:

Thiazolidinyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, optionally substituted on the thiazolidine ring with one or two members selected from the group consisting of an oxo group and a thioxo group;

such as 2 - [(2-, 3-, 4-, or 5-) thiazolidinyl] acetyl, 3 - [(2-, 3-, 4-, or

5-) thiazolidinyl] propionyl, 2 - [(2-, 3-, 4-, or 5-) thiazolidinyl] propionyl, 4 - [(2-, 3-, 4-, or 5-) thiazolidinyl] butyryl, 5- [ (2-, 3-, 4-, or 5-) thiazolidinyl] pentanoyl, 6 - [(2-,

3-, 4-, or 5-) thiazolidinyl] hexanoyl, 2,2-dimethyl-3 - [(2-, 3-, 4-, or 5-) thiazolidinyl] propionyl, 2-methyl-3 - [(2 -, 3-, 4-, or 5-) thiazolidinyl] propionyl, [2-thioxo-4-oxo-2- (3- or 5-) thiazolidinyl] acetyl, [2-thioxo-2- (3-, 4 -, or 5-) thiazolidinyl] acetyl, [2-oxo]

2- (3-, 4-, or 5-) thiazolidinyl] acetyl, [2,4-dithioxo-2- (3- or 5-) thiazolidinyl] acetyl, and [2,4-dioxo-2- (3- or 5-) thiazolidinyl] acetyl.

Examples of lower piperidinyl alkanoyl groups include piperidinyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group such as 2 - [(1-, 2-, 3-, or 4-) piperidinyl] acetyl , 3 - [(1-, 2-,

3-, or 4-) piperidinyl] propionyl, 2 - [(1-, 2-, 3-, or 4-) piperidinyl] propionyl, 4- [(1-, 2-, 3-, or 4-) piperidinyl ] butyryl, 5 - [(1-, 2-, 3- or 4-) piperidinyl] pentanoyl,

6 - [(1-, 2-, 3-, or 4-) piperidinyl] hexanoyl, 2,2-dimethyl-3 - [(1-, 2-, 3-, or 4-) piperidinyl] propionyl, and 2-methyl-3 - [(1-, 2-, 3-, or 4-) piperidinyl] propionyl.

Examples of phenyl alkenylcarbonyl groups optionally substituted on the phenyl ring with one or more halogen atoms include: phenyl alkenylcarbonyl groups containing one to three double bonds.

plasmas wherein the alkenyl moiety is a straight or branched C 2-6 alkenyl group, optionally substituted on the phenyl ring with one to three halogen atoms;

Such as styrylcarbonyl (trivial name: cinnamoyl group), 3-phenyl-2-propenylcarbonyl, 4-phenyl-2-butenylcarbonyl, 4-phenyl-3-butenylcarbonyl, 5-phenyl-4-pentenylcarbonyl, 5-phenyl-3 -pentenylcarbonyl, 6-phenyl-5-hexenylcarbonyl, 6-phenyl-4-hexenylcarbonyl, 6-phenyl-3-hexenylcarbonyl, 4-phenyl-1,3-butadienylcarbonyl, 6-phenyl-1,3,5-hexatrienylcarbonyl 2,2-Chlorostyrylcarbonyl, 3- (4-bromophenyl) -2-propenylcarbonyl, 4- (3-fluorophenyl) -2-butenylcarbonyl, 4- (2,4-dichlorophenyl) -3-butenylcarbonyl, 5- ( 2,4,6-trifluorophenyl) -4-pentenylcarbonyl, 5- (4-io-dophenyl) -3-pentenylcarbonyl, 6- (3-chlorophenyl) -5-hexenylcarbonyl, 6- (4-chloro-phenyl) -4 -hexenylcarbonyl, 6- (3,4-dichlorophenyl) -3-hexenylcarbonyl, 4- (3-chloro-4-fluorophenyl) -1,3-butadienylcarbonyl, and 6- (2,6-difluorophenyl) -1,3, 5-hexatrienylcarbonyl.

Examples of phenyl lower alkenylcarbonyl groups optionally substituted on the phenyl ring with one or more lower alkylenedioxy groups include:

Phenyl alkenylcarbonyl groups containing one to three double bonds wherein the alkenyl moiety is a straight or branched C2- and alkenyl group, optionally substituted on the phenyl ring with one or more of the linear or branched C1-4 alkylenedioxy groups described above;

such as 3,4-methylenedioxystyrylcarbonyl, 3- (2,3-ethylenedioxyphenyl) -2-propenylcarbonyl, 4- (3,4-trimethylenedioxyphenyl) -2-butenylcarbonyl, 4- (2,3-tetramethylenedioxyphenyl) -3- butenylcarbonyl, 5- (2,3-methylenedioxyphenyl) -4-pentenylcarbonyl, 5- (3,4-ethylenedioxyphenyl) -3-pentenylcarbonyl, 6- (2,3-trimethylene dioxiphenyl) -5-hexenylcarbonyl, 6- (3,4-tetramethylenedioxyphenyl) -4-hexenylcarbonyl, 6- (2,3-methylenedioxyphenyl) -3-hexenylcarbonyl, 4- (3,4-methylenedioxyphenyl) -1,3-butadienylcarbonyl, and 6- (2, 3-methylenedioxyphenyl) -1,3,5-hexatrienylcarbonyl.

Examples of pyridyl lower alkenylcarbonyl groups include pyridyl alkenylcarbonyl groups containing one to three double bonds wherein the alkenyl moiety is a straight or branched C2- and alkenyl group, such as 2 - [(2-, 3-, or 4-) pyridyl] vinylcarbonyl, 3 - [(2-, 3-, or 4-) pyridyl] -2-propenylcarbonyl, 4 - [(2-, 3-, or 4-) pyridyl] -2-butenylcarbonyl, 4- [(2-, 3-, or 4-) pyridyl] -

3-Butenylcarbonyl, 5 - [(2-, 3- or 4-) pyridyl] -4-pentenyl carbonyl, 5 - [(2-, 3-, or

4-) pyridyl] -3-pentenylcarbonyl, 6 - [(2-, 3-, or 4-) pyridyl] -5-hexenylcarbonyl, 6- [(2-, 3-, or 4-) pyridyl] -4- hexenylcarbonyl, 6 - [(2-, 3-, or 4-) pyridyl] -3-hexenylcarbonyl, 4-phenyl-1,3-butadienylcarbonyl, and 6 - [(2-, 3-, or 4-) pyridyl] - 1,3,5-hexatrienylcarbonyl.

Examples of lower pyridylthio alkanoyl groups include pyridylthio alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, such as 2 - [(2-, 3-, or 4-) pyridylthio] acetyl, 3 - [( 2-, 3-, or 4-) pyridylthio] propionyl, 2 - [(2-, 3-, or 4-) pyridylthio] propionyl, 4 - [(2-, 3-, or 4-) pyridylthio] butyryl, 5 - [(2-, 3-, or 4-) pyridylthio] pentanoyl, 6 - [(2-, 3-, or 4-) pyridylthio] hexanoyl, 2,2-dimethyl-3 - [(2-, 3 -, or 4-) pyridylthio] propionyl, and 2-methyl-3 - [(2-, 3-, or 4-) pyridylthio] propionyl.

Examples of indolylcarbonyl groups include 1-indolylcarbonyl,

2-indolylcarbonyl, 3-indolylcarbonyl, 4-indolylcarbonyl, 5-indolylcarbonyl, 6-indolylcarbonyl, and 7-indolylcarbonyl.

Examples of pyrrolylcarbonyl groups include 2-pyrrolylcarbonyl and

3-pyrrolylcarbonyl.

Examples of pyrrolidinylcarbonyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups include pyrrolidinylcarbonyl groups optionally substituted on the pyrrolidine ring with one or two oxo groups, such as (1-, 2-, or 3-) pyrrolidinylcarbonyl, 2 -oxo- (1-, 3-, 4-, or

5-) pyrrolidinylcarbonyl, 3-oxo- (1-, 2-, 4-, or 5-) pyrrolidinylcarbonyl, 2,5-dioxo- (1- or 3-) pyrrolidinylcarbonyl, and 2,3-dioxo- (1- , 4-, or 5-) pyrrolidinylcarbonyl.

Examples of benzofurylcarbonyl groups include 2-benzofurylcarbonyl, 3-benzofurylcarbonyl, 4-benzofurylcarbonyl, 5-benzofurylcarbonyl, 6-benzofurylcarbonyl, and 7-benzofurylcarbonyl.

Examples of lower indolyl alkanoyl groups include indolyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, such as 2 - [(1-, 2-, 3-, 4-, 5-, 6 -, or 7-) indolyl] acetyl, 3 - [(1-, 2-, 3-, 4-, 5-, 6-, or 7-) indolyl] propionyl, 2 - [(1-, 2-, 3- , 4-, 5-, 6-, or 7-) indolyl] propionyl, 4 - [(1-, 2-, 3-, 4-, 5-, 6-, or 7-) indolyl] butyryl, 5 - [(1-, 2-, 3-, 4-, 5-,

6-, or 7-) indolyl] pentanoyl, 6 - [(1-, 2-, 3-, 4-, 5-, 6-, or 7-) indolyl] hexanoyl, 2,2-dimethyl-3- [ (1-, 2-, 3-, 4-, 5-, 6-, or 7-) indolyl] propionyl, and 2-methyl-3 - [(1-, 2-, 3-, 4-, 5-, 6 -, or 7-) indolylpropionyl.

Examples of benzothienylcarbonyl groups include 2-benzothienylcarbonyl, 3-benzothienylcarbonyl, 4-benzothienylcarbonyl, 5-benzothienylcarbonyl, 6-benzothienylcarbonyl, and 7-benzothienylcarbonyl.

Examples of phenyl lower alkanoyl groups optionally substituted on the phenyl ring with one or more halogen atoms include:

Phenyl alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, optionally substituted on the phenyl ring with one to three halogen atoms;

Such as 2-phenylacetyl, 3-phenylpropionyl, 2-phenylpropionyl, 4-phenylbutyryl, 5-phenylpentanoyl, 6-phenylhexanoyl, 2,2-dimethyl-3-phenylpropionyl, 2-methyl-3-phenylpropionyl, 2- (4-fluorophenyl ) acetyl, 3- (2,5-difluorophenyl) propionyl, 2- (2,4-difluorophenyl) propionyl, 4- (3,4-difluorophenyl) butyryl, 5- (3,5-difluorophenyl) pentanoyl, 6 - (2,6-difluorophenyl) hexanoyl, 2- (2-chlorophenyl) acetyl, 3- (3-chlorophenyl) propionyl, 2- (4-chlorophenyl) propionyl, 4- (2,3-dichlorophenyl) propionyl, 5- (2,4-dichlorophenyl) pentanoyl, 6- (2,5-dichlorophenyl) hexanoyl, 2- (3,4-dichlorophenyl) acetyl, 3- (2,6-dichlorophenyl) propionyl, 2- (3-fluorophenyl ) propionyl, 4- (2-fluorophenyl) butyryl, 5- (3-bromophenyl) pentanoyl, 6- (4-iodophenyl) hexanoyl, 2- (2-bromophenyl) acetyl, 3- (4-bromophenyl) propionyl, 2- (3,5-dichlorophenyl) propionyl, 4- (2,4,6-trifluorophenyl) butyryl, 5- (3,4-difluorophenyl) pentanoyl, 6- (2-iodophenyl) hexanoyl, 2- (3-iodophenyl) acetyl, 3- (4-iodophenyl) propionyl, 2- (2 , 3-dibromophenyl) propionyl, 4- (2,4-diodophenyl) butyryl, and 2- (2,4,6-trichlorophenyl) acetyl.

Examples of phenylsulfonyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxycarbonyl groups; a cyan group; a nitro group; nitro groups optionally substituted with one or more lower alkanoyl groups; a hydroxy group; a carboxyl group; lower alkyl lower alkoxycarbonyl groups; halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; and lower alkoxy groups optionally substituted with one or more halogen atoms include:

Phenylsulfonyl groups optionally substituted on the phenyl ring having one or five members selected from the group consisting of the lower alkoxycarbonyl groups described above wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group; a cyan group; a nitro group; those described above amino groups optionally substituted with one or two straight and / or branched C 1-6 alkanoyl groups; a hydroxy group; a carboxyl group; the alkoxycarbonylalkyl groups described above wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group and the alkyl moiety is a straight or branched C 1-6 alkyl group; halogen atoms; the above described linear and branched C1-6 alkyl groups optionally substituted with one to three halogen atoms; and the above described linear and branched C1-6 alkoxy groups optionally substituted with one to three halogen atoms;

such as phenylsulfonyl, 4-methoxyphenylsulfonyl, 3-methoxyphenylsulfonyl, 2-methoxyphenylsulfonyl, 2-trifluoromethoxyphenylsulfonyl, 3-trifluoromethoxyphenylsulfonyl, 3,4-dimethylsulfonyl, 2,4-dimethoxyphenyl trimethoxyphenylsulfonyl, 4-n-butoxyphenylsulfonyl, 2-methoxy-5-chlorophenylsulfonyl, 2-methoxy-5-methylphenylsulfonyl, 2-methoxy-4-methylphenylsulfonyl, 4-chlorophenylsulfonyl, 2-chlorophenylsulfonyl, 2-chlorophenylsulfonyl 3-fluorophenylsulfonyl, 2-fluorophenylsulfonyl, 4-bromophenylsulfonyl, 3-bromophenylsulfonyl, 2-bromophenylsulfonyl, 2,6-dichlorophenylsulfonyl, 2,3-dichlorophenylsulfonyl, 2,5-dichlorophenylsulfonyl, 2,4-dichlorophenyl, dichlorophenylsulfonyl, 3,5-dichlorophenylsulfonyl, 2-chloro-4-fluorophenylsulfonyl, 2-bromo-5-chlorophenylsulfonyl, 2,5-difluorophenylsulfonyl, 2,4-difluorophenylsulfonyl, 2,6-difluorophenylsulfonyl, 3,4-difluorophenylsulfonyl 4-dichloro-5-methylphenyl sulfo nyl, 2,4,5-trifluorophenylsulfonyl, 2,3,4,5,6-pentafluorophenylsulfonyl, 3-chloro-4-fluorophenylsulfonyl, 2-chloro-6-methylphenylsulfonyl, 2,4-dichloro-6-methylphenylsulfonyl, 2-methyl-3-chlorophenylsulfonyl, 2-methyl-3-chlorophenylsulfonyl, A-methyl-3-chlorophenylsulfonyl, 2-methyl-5-fluorophenylsulfonyl, methyl-4-bromophenylsulfonyl, 2-fluoro-4-bromophenylsulfonyl, 2 , 5-dimethyl-4-chlorophenylsulfonyl, 2-methylphenylsulfonyl, 3-methylphenylsulfonyl, 4-methylphenylsulfonyl, 2,5-dimethylphenylsulfonyl, 2,4,6-trimethylphenylsulfonyl, 2,3,6-trimethyl-4-methoxyphenylsulfonyl, A - tert-butylphenylsulfonyl, 4-ethylphenylsulfonyl, 4-isopropylphenylsulfonyl, 2-trifluoromethylphenylsulfonyl, 3-trifluoromethylphenylsulfonyl, 4-trifluoromethylphenylsulfonyl, 2-cyanophenylsulfonylsulfonyl, 3-trifluoromethylphenylsulfonyls , 4-nitrophenyl sulfonyl, 3-nitro-4-methylphenylsulfonyl, 3-nitro-6-methylphenylsulfonyl, 3-nitro-6-chlorophenyl 1sulfonyl, 2-chloro-4-cyanophenylsulfonyl, 4-acetylaminophenylsulfonyl, 3-chloro-4-acetylaminophenylsulfonyl, 2-hydroxy-3,5-dichlorophenylsulfonyl, 2-hydroxyphenylsulfonyl, 4-hydroxyphenylsulfonyl 4-Methoxyphenylsulfonyl, 3-carboxyphenylsulfonyl, 4-carboxyphenylsulfonyl, 2-carboxyphenylsulfonyl, 4- (2-methoxycarbonylethyl) phenylsulfonyl, 3-carboxy-4-hydroxyphenylsulfonyl, 3-aminophenylsulfonyl, 2-aminophenyl, and 4-aminophenylsulfonyl aminophenylsulfonyl.

Examples of thienylsulfonyl groups optionally substituted on the thiophene ring with one or more members selected from the group consisting of halogen atoms and lower alkoxycarbonyl groups include:

Thienylsulfonyl groups optionally substituted on the thiophene ring having one to three members selected from halogen atoms and the alkoxycarbonyl groups described above wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group;

such as (2- or 3-) thienylsulfonyl, [2-chloro- (3-, 4-, or 5-) thienylsulfonyl, [2,3-dichloro- (4- or 5-) thienylsulfonyl, [2, 5-dichloro- (3- or 4-) thienylsulfonyl, [2-bromo- (3-, 4-, or 5-) thienylsulfonyl, [2-fluoro- (3-, 4-, or 5-) thienylsulfonyl , (2,3,4-trichloro-5-thienyl) sulfonyl, [2-methoxycarbonyl- (3-, 4-, or 5-) thienylsulfonyl, [3-ethoxycarbonyl- (2-, 4-, or 5-) thienylsulfonyl, [3- / 7-propoxycarbonyl- (2-, 4-, or 5-) thienylsulfonyl, [2-tert-butoxycarbonyl- (3-, 4-, or 5-) thienylsulfonyl, [2-n-pentyloxycarbonyl] (3-, 4-, or 5-) thienyl] sulfonyl, [3-n-hexyloxycarbonyl- (2-, 4-, or 5-) thienyl] sulfonyl, [2,3-dimethoxycarbonyl- (4- or 5-) thienyl] sulfonyl, and [2-chloro-3-methoxycarbonyl- (4- or 5-) thienyl] sulfonyl.

Examples of quinolylsulfonyl groups include 2-quinolylsulfonyl,

3-quinolylsulfonyl, 4-quinolylsulfonyl, 5-quinolylsulfonyl, 6-quinolylsulfonyl, 7-quinolylsulfonyl, and 8-quinolylsulfonyl.

Examples of imidazolylsulfonyl groups optionally substituted on the imidazole ring with one or more lower alkyl groups include imidazolylsulfonyl groups optionally substituted on the imidazole ring with one to three linear or branched C1-6 alkyl groups described above, such as (1-, 2-,

4-, or 5-) imidazolylsulfonyl, [1-methyl- (2-, 4-, or 5-) imidazolyl] sulfonyl, [2-ethyl- (1-, 4-, or 5-) imidazolyl] sulfonyl, [1-isopropyl] (2-, 4-, or 5-) imidazole

Lysulfonyl, [4- n -butyl- (1-, 2-, or 5-) imidazolyl] sulfonyl, [5-7-pentyl- (1-, 2-, or 4-) imidazolyl] sulfonyl, [1- [hexyl] (2-, 4-, or 5-) imidazolyl] sulfonyl, [1,2-dimethyl- (4- or 5-) imidazolyl] sulfonyl, and (1,2,4-trimethyl-5-imidazolyl) sulfonyl.

Examples of phenylsulfonyl groups optionally substituted on the phenyl ring with one or more lower alkylenedioxy groups include phenylsulfonyl groups optionally substituted on the phenyl ring with one or more linear or branched C1-4 alkylenedioxy groups described above, such as (3,4-ethylenedioxyphenyl) sulfonyl, (2,3-methylenedioxyphenyl) sulfonyl, (3,4-trimethylenedioxyphenyl) sulfonyl, and (2,3-tetramethylenedioxyphenyl) sulfonyl.

Examples of lower alkenylsulfonyl groups include straight and branched C 2-6 alkenylsulfonyl groups containing one to three double bonds, such as vinylsulfonyl, 1-propenylsulfonyl, "1-methyl-1-propenylsulfonyl, 2-methyl-1-propenylsulfonyl, 2-propenylsulfonyl, 2-butenylsulfonyl, 1-butenylsulfonyl, 3-butenylsulfonyl, 2-pentenylsulfonyl, 1-pentenylsulfonyl, 3-pentenylsulfonyl, 4-pentenylsulfonyl, 1,3-butadienylsulfonyl, 1,3-pentadienylsulfonyl, 2-pentene-4-one inylsulfonyl, 2-hexenylsulfonyl, 1-hexenylsulfonyl, 5-hexenylsulfonyl, 3-hexenylsulfonyl, 4-hexenylsulfonyl, 3,3-dimethyl-1-propenylsulfonyl, 2-ethyl-1-propenylsulfonyl, 1,3,5-hexatrienylsulfonyl, 1,3-hexadienylsulfonyl, and 1,4-hexadienylsulfonyl.

Examples of cycloalkyl substituted lower alkylsulfonyl groups include C 3-8 cycloalkyl substituted alkylsulfonyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as cyclopropylmethylsulfonyl, cyclohexylmethylsulfonyl, 2-cyclopropylethylsulfonyl, 1-cyclobutylethylsulfonyl, cyclopentyl , 3-cyclopentylpropylsulfonyl, 4-cyclohexylbutylsulfonyl, 5-cycloheptylpentylsulfonyl, 6-cyclooctylhexylsulfonyl, 1,1-dimethyl-2-cycloheethylethylsulfonyl, and 2-methyl-3-cyclopropylpropylsulfonyl.

Examples of optionally substituted 3,4-dihydro-2H-1,4-benzoxazinylsulfonyl groups on the 3,4-dihydro-2H-1,4-benzoxazine ring having one or more lower alkyl groups include 3,4-dihydroxy groups. Optionally substituted 2H-1,4-benzoxazinylsulfonyl ring 3,4-dihydro-2H-1,4-benzoxazine having one to three linear and / or branched C1-6 alkyl groups described above, such as (2- , 3-, 4-, 5-, 6-, 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinylsulfonyl, [4-methyl- (2-, 3-, 5-, 6- , 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinyl] sulfonyl, [5-ethyl- (2-, 3-, 4-, 6-, 7- or 8-) 3,4 -dihydro-2H-1,4-benzoxazinyl] sulfonyl, [6-n-propyl- (2-, 3-, 4-, 5-, 7- or 8-) 3,4-dihydro-2H-1,4 - benzoxazinyl] sulfonyl, [7-n-butyl- (2-, 3-, 5-, 6-, 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinyl] sulfonyl, [8- n-pentyl- (2-, 3-, 5-, 6-, 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinyl] sulfonyl, [2-n-hexyl- (3-, 4-, 5-, 6-, 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinyl] sulfonyl, [3-methyl- (2-, 4-, 5-, 6-, 7 - or 8-) 3,4-dihydro-2H-1,4-benzoxazol nyl] sulfonyl, [4,6-dimethyl- (2-, 3-, 5-, 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinyl] sulfonyl, and [4,5,6 -trimethyl- (2-, 3-, 7- or 8-) 3,4-dihydro-2H-1,4-benzoxazinyl] sulfonyl.

Examples of pyrazolylsulfonyl groups optionally substituted on the pyrazole ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups include:

Pyrazolylsulfonyl groups optionally substituted on the one to three membered pyrazole ring selected from the group consisting of halogen atoms and the linear and branched C1-6 alkyl groups described above;

such as (1-, 3-, 4-, or 5-) pyrazolylsulfonyl, (1,3-dimethyl-5-chloro-

4-pyrazolyl) sulfonyl, [1-ethyl- (3-, 4-, or 5-) pyrazolyl] sulfonyl, [3-n-propyl- (1-, 4-, or 5-) pyrazolyl] sulfonyl, [4 -n-butyl- (3-, 4-, or 5-) pyrazolylsulfonyl, [5-n-pentyl- (1-, 3-, or 4-) pyrazolylsulfonyl, [1-n-hexyl- (3-, 4 -, or 5-) pyrazolylsulfonyl, [1,3-dimethyl- (4- or 5-) pyrazolylsulfonyl, (1,3,5-trimethyl-4-pyrazolyl) sulfonyl, [3-bromo- (1-, 4- , or 5-) pyrazolylsulfonyl, [4-fluoro- (1-, 3-, or 5-) pyrazolylsulfonyl, [5-iodo- (1-, 3-, or 4-) pyrazolylsulfonyl, [3,4- dichloro- (1- or 5-) pyrazolyl] sulfonyl, and (3,4,5-trichloro-4-pyrazolyl) sulfonyl.

Examples of isoxazolylsulfonyl groups optionally substituted on the isoxazole ring with one or more lower alkyl groups include isoxazolylsulfonyl groups optionally substituted on the isoxazole ring with one or two C1-6 straight and / or branched alkyl groups described above, such as (3-4) -, or 5-) isoxazolylsulfonyl, (3,5-dimethyl-4-isoxazolyl) sulfonyl, [3-methyl- (4- or 5-) isoxazolylsulfonyl, [3-ethyl- (4- or 5-) isoxazolyl] sulfonyl , [4-n-propyl- (3- or 5-) isoxazolylsulfonyl, [5-n-butyl- (3- or 4-) isoxazolylsulfonyl], [3-n-pentyl- (4- or 5-) isoxazolyl] sulfonyl , and [4-n-hexyl- (3- or 5-) isoxazolyl] sulfonyl.

Examples of thiazolylsulfonyl groups optionally substituted on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and one amino group, each amino substituent optionally being substituted with one or more lower alkanoyl groups, include:

Optionally substituted thiazolylsulfonyl groups on the triazole ring having one or two members selected from the group consisting of the linear or branched C1-6 alkyl groups described above and the above described amino groups optionally substituted with one or two C1-6 linear alkanoyl groups and / or branched;

such as (2-, 4-, or 5-) thiazolylsulfonyl, (2-acetylamino-4-methyl-5-thiazolyl) sulfonyl, [2-ethyl- (4- or 5-) thiazolyl] sulfonyl, [4-n -propyl- (2- or 5-) thiazolylsulfonyl, [5-n-butyl- (2- or 4-) thiazolyl] sulfonyl, [2-n-pentyl- (4- or 5-) thiazolyl] sulfonyl, [4-n-hexyl- (2- or 5-) thiazolylsulfonyl, (2,4-dimethyl-5-thiazolyl) sulfonyl, [2-amino- (4- or 5-) thiazolyl] sulfonyl, [2- formylamino- (4- or 5-) thiazolyl] sulfonyl, [4-n-propionylamino- (2- or 5-) thiazolyl] sulfonyl, [5-n-butyryl amino- (2- or 4-) thiazolyl] sulfonyl, [2-n-pentanoylamino- (4- or 5-) thiazolyl] sulfonyl, [4- n-hexanoylamino- (2- or 5-) thiazolyl] sulfonyl, (2,4-diacetyl-5-thiazolyl) sulfonyl, and [2 - ([V, [V-diacetylamino) - (4- or 5-) thiazolyl] sulfonyl.

Examples of phenyl lower alkylsulfonyl groups include mono- and di-phenylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as benzylsulfonyl, 1-phenylsulfonyl, 2-phenylsulfonyl, 3-phenylpropylsulfonyl, 2-phenylpropylsulfonyl, 4-phenylbutylsulfonyl, 5-phenylpentylsulfonyl, 4-phenylpentylsulfonyl, 6-phenylhexylsulfonyl, 2-methyl-3-phenylpropylsulfonyl, 1,1-dimethyl-2-phenylethylsulfonyl, 1,1-dimethyl-1-phenylmethylsulfonyl, 1, 1-diphenylmethylsulfonyl, 2,2-diphenylethylsulfonyl, 3,3-diphenylpropylsulfonyl, and 1,2-diphenylethylsulfonyl.

Examples of phenyl lower alkenylsulfonyl groups include: phenylalkenylsulfonyl groups containing one to three double bonds wherein the alkenyl moiety is a straight or branched C 2-6 alkenyl group, optionally substituted on the phenyl ring with one to three halogen atoms;

such as styrylsulfonyl, 3-phenyl-2-propenylsulfonyl, 4-phenyl-2-butenylsulfonyl, 4-phenyl-3-butenylsulfonyl, 5-phenyl-4-pentenylsulfonyl, 5-phenyl-3-pentenylsulfonyl, 6-phenyl-5-one hexenylsulfonyl, 6-phenyl-4-hexenylsulfonyl, 6-phenyl-3-hexenylsulfonyl, 4-phenyl-1,3-butadienylsulfonyl, 6-phenyl-1,3,5-hexatrienylsulfonyl, 2-chlorostyrylsulfonyl, 3- (4) -bromophenyl) -2-propenylsulfonyl, 4- (3-fluorophenyl) -2-butenylsulfonyl, 4- (2,4-dichlorophenyl) -3-butenylsulfonyl, 5- (2,4,6-trifluorophenyl) - 4-pentenylsulfonyl, 5- (4-iodophenyl) -3-pentenylsulfonyl, 6- (3-chlorophenyl) -5-hexenylsulfonyl, 6- (4-chlorophenyl) -4-hexenylsulfonyl, 6- (3,4-dichlorophenyl ) - 3-hexenylsulfonyl, 4- (3-chloro-4-fluorophenyl) -1,3-butadienylsulfonyl, and 6- (2,6-difluorophenyl) -1,3,5-hexatrienylsulfonyl.

Examples of naphthyloxycarbonyl groups include 1-naphthyloxycarbonyl and 2-naphthyloxycarbonyl.

Examples of alkynyloxycarbonyl include alkynyloxycarbonyl groups wherein the alkynyl moiety is a C 2-6 Inear or branched alkynyl group such as ethinyloxycarbonyl, 2-propynyloxycarbonyl, 2-butynyloxycarbonyl, 3-butynyloxycarbonyl, 1-methyl-2-propynyloxycarbonyl 2-pentinyloxycarbonyl, and 2-hexinyloxycarbonyl.

Examples of lower alkenyloxycarbonyl groups include alkenyloxycarbonyl groups containing one to three double bonds wherein the alkenyl moiety is a straight or branched C2-6 alkenyl group such as vinyloxycarbonyl, 1-propenyloxycarbonyl, 1-methyl-1-propenyloxycarbonyl, 2- methyl-1-propenyloxycarbonyl, 2-propenyloxycarbonyl, 2-butenyloxycarbonyl, 1-butenyloxycarbonyl, 3-butenyloxycarbonyl, 2-pentenyloxycarbonyl, 1-pentenyloxycarbonyl, 3-pentenyloxycarbonyl, 4-pentenyloxycarbonyl, 1,3-butoxycarbonyl 1,3-pentadienyloxycarbonyl, 2-pentene-4-ynyloxycarbonyl, 2-hexenyloxycarbonyl, 1-hexenyloxycarbonyl, 5-hexenyloxycarbonyl, 3-hexenyloxycarbonyl, 4-hexenyloxycarbonyl, 3,3-dimethyl-1-propenyloxycarbonyl, 2- ethyl-1-propyloxycarbonyl, 1,3,5-hexatrienyloxycarbonyl, 1,3-hexadienyloxycarbonyl, and 1,4-hexadienyloxycarbonyl.

Examples of phenyl lower alkoxy substituted lower alkoxycarbonyl groups include phenylalkoxy substituted alkoxycarbonyl groups wherein each of the two alkoxy moieties is a straight or branched C1-6 alkoxy group such as phenylmethoxymethoxycarbonyl, 2- (phenylmethoxy) ethoxycarbonyl, 1- (phenylmethoxy) ethoxycarbonyl, 3- (phenylmethoxy) propoxycarbonyl, 4- (phenylmethoxy) butoxycarbonyl, 5- (phenylmethoxy) pentyloxycarbonyl, 6- (phenylmethoxy) hexyloxycarbonyl, 1,1-dimethyl-2- (phenylmethoxy) ethoxycarbonyl, 2- methyl-3- (phenylmethoxy) propoxycarbonyl, 1- (2-phenylethyloxy) ethoxycarbonyl, 2- (1-phenylethyloxy) ethoxycarbonyl, 3- (3-phenylpropoxy) propoxycarbonyl, 4- (4-phenylbutoxy) butoxycarbonyl, 5- ( 5-phenylpentyloxy) pentyloxycarbonyl, 6- (6-phenylhexyloxy) hexyloxycarbonyl, 1,1-dimethyl-2-phenylethyloxy) methoxycarbonyl, and 3- (2-methyl-3-phenylpropoxy) propoxycarbonyl.

Examples of cycloalkyloxycarbonyl groups optionally substituted on the cycloalkyl ring with one or more lower alkyl groups include: Cycloalkyloxycarbonyl groups wherein the cycloalkoxy moiety is a

C 3-8 cycloalkoxy group, optionally substituted on the cycloalkyl ring with one to three linear or branched C 1-6 alkyl groups described above;

such as cyclopropyloxycarbonyl, cyclobutyloxycarbonyl, cyclopentyloxycarbonyl, cyclohexyloxycarbonyl, cycloeptyloxycarbonyl, cyclooctyloxycarbonyl, 3-methyl-6-isopropylcyclohexylcarbonyl, 2-ncyclopropyloxycarbonylcyclyloxycarbonyl, 3-methylpropyloxycarbonyl 2-methylcyclopentyloxycarbonyl, and 2,3,6-trimethylcycloexyloxycarbonyl.

Examples of isoxazolyl groups optionally substituted on the isoxazole ring with one or more lower alkyl groups include isoxazolyl groups optionally substituted on the isoxazole ring with one or two linear and / or branched C1-6 alkyl groups, such as (3-, 4-, or 5-) isoxazolyl, 5-methyl- (3- or 4-) isoxazolyl, 3,5-dimethyl-4-isoxazolyl, 3-ethyl- (4- or 5-) isoxazolyl, 4-n-propyl (3- or 5-) isoxazolyl, 5-n-butyl- (3- or 4-) isoxazolyl, 3-n-pentyl- (4- or 5-) isoxazolyl and 4-n-hexyl- (3- or 5) -) isoxazolyl.

Examples of 5- to 7-membered saturated heterocyclic rings formed of R 6 and R 7 being attached together, together with the nitrogen atom to which they are attached, the heterocyclic ring optionally containing one or more additional heteroatoms, include: Saturated heterocyclic rings of 5 to 7 members formed from

R 6 and R 7 being bonded together, together with the nitrogen atom to which they are attached, the heterocyclic group optionally containing one or more additional heteroatoms selected from nitrogen atom, sulfur atom and oxygen;

such as pyrrolidine, piperazine, piperidine, morpholine, thiomorpholine

na, homopiperazine, homopiperidine, imidazolidine, thiazolidine, isothiazolidine, oxazolidine, isoxazolidine, isothiazolidine, and pyrazolidine. Examples of phenyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms; lower alkoxy groups optionally substituted with one or more halogen atoms; lower alkyl groups optionally substituted with one or more halogen atoms; a cyan group; and a hydroxy group include:

Optionally substituted phenyl groups on the phenyl ring having one to three members selected from the group consisting of halogen atoms; the above described linear and branched C1-6 alkoxy groups optionally substituted with one to three halogen atoms; in the above described straight and branched C 1-6 alkyl groups optionally substituted with one to three halogen atoms; a cyan group; and a hydroxy group;

such as phenyl, 4-isopropylphenyl, 3-isopropylphenyl, 2-isopropylphenyl, 4-tert-butylphenyl, 4-methylphenyl, 3-methylphenyl, 2-methylphenyl, 2,3-dimethylphenyl, 2,4-dimethylphenyl, 3,5-dimethylphenyl, 2,4,6-trimethylphenyl, 4-methyl-3-methoxyphenyl, 4-trifluoromethylphenyl, 3-trifluoromethylphenyl, 2-trifluoromethylphenyl, 4-methyl-3-chlorophenyl, 4-chlorophenyl, 3- chlorophenyl, 2-chlorophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-bromophenyl, 3,4-dichlorophenyl, 3,5-dichlorophenyl, 3,4,5-trichlorophenyl, 2,4,6-trifluorophenyl, 3,5-difluorophenyl, 3-chloro-4-fluoro-phenyl, 2-chloro-5-fluorophenyl, 3-fluoro-4-methoxyphenyl, 3-chloro-4-methoxyphenyl, 3-chloro-4-hydroxyphenyl, 4- methoxyphenyl, 3-methoxyphenyl, 2-methoxyphenyl, 2,4-dimethoxyphenyl, 3,4-dimethoxyphenyl, 2,4,6-trimethoxyphenyl, 2-methoxy-5-chlorophenyl, 4-ethoxyphenyl, 4-trifluoromethoxyphenyl, 3-trifluoromethoxyphenyl 2-trifluoromethoxyphenyl, 3-methoxy-5-trifluoromethylphenyl, 2-cyanophenyl, 3-cyanophenyl, 4-cyanophenyl, 3-hydro xiphenyl, 2-hydroxyphenyl, and 4-hydroxyphenyl.

Examples of optionally substituted lower alkyl phenyl groups on the phenyl ring having one or more halogen atoms include:

Mono- and di-phenylalkyl groups wherein the allyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on each phenyl ring having one to three halogen atoms;

such as benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenylhexyl, 2-methyl-3-phenylpropyl, 1, 1-dimethyl-2-phenylethyl, 1,1-diphenylmethyl, 2,2-diphenylethyl, 3,3-diphenylpropyl, 1,2-diphenylethyl, 4-chlorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 2-fluoro robenzyl, 3-fluorobenzyl, 4-fluorobenzyl, 2,3-dichlorobenzyl, and 2,4,6-trifluorobenzyl.

Examples of optionally substituted phenyl lower alkoxy groups

phenyl ring having one or more halogen atoms include:

Phenylalkoxy groups wherein the alkoxy moiety is a straight or branched C 1-6 alkoxy group, optionally substituted on the phenyl ring with one to three halogen atoms; such as benzyloxy, 2-phenylethyloxy, 1-phenylethyloxy, 3-phenylpropoxy, 4-

phenylbutoxy, 5-phenylpentyloxy, 6-phenylhexyloxy, 1,1-dimethyl-2-phenylethyloxy, 2-methyl-3-phenylpropoxy, 4-chlorobenzyloxy, 2-chlorobenzyloxy, 3-chlorobenzyloxy, 2-fluorobenzyloxy, 3-fluorobenzyloxy, 4-fluorobenzyloxy, 2,4-dibromobenzyloxy, and 2,4,6-trifluorobenzyloxy.

Examples of optionally lower carbamoyl alkyl groups

Substituted with one or more members selected from the group consisting of phenyl and lower alkyl groups include:

Carbamoylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted with one or two members selected from the group consisting of a phenyl group and the branched and straight C 1-6 alkyl groups described above;

such as carbamoylmethyl, 2-carbamoylethyl, 1-carbamoylethyl, 3-carbamoylpropyl, 4-carbamoylbutyl, 5-carbamoylpentyl, 6-carbamoylhexyl, 1,1-dimethyl-2-carbamoylethyl, 2-methyl-3-carbamoylpropyl, 2- (A t-methyl-Î ± -phenylcarbamoyl) ethyl, β-phenylcarbamoylmethyl, 2- (β-V-dimethylcarbamoyl) ethyl, 3- (N-phenylcarbamoyl) propyl, 2- (Î ± -ethyl-A / (phenylcarbamoyl) ethyl, N, N -dimethylcarbamoylmethyl, N-methyl-N / ethylcarbamoylmethyl, N-methylcarbamoylmethyl, and 2- (N-methylcarbamoyl) ethyl.

Examples of optionally substituted phenyl lower alkylidene groups on the phenyl ring having one or more halogen atoms include:

Phenylalkylidene groups wherein the alkylidene moiety is a straight or branched C1-6 alkylidene group, optionally substituted on the phenyl ring with one to three halogen atoms;

such as phenylmethylidene, phenylethylidene, phenylpropylidene, phenylisopropylidene, phenylbutylidene, phenylpentylidene, phenylhexylidene, 2-chlorophenylmethylidene, 4-chlorophenylmethylidene, 2-fluorophenylmethylene, 4-chlorophenylmethylidene bromophenylmethylidene, 4-bromophenylmethylidene, 2-iodophenylmethylidene, 2,3-dichlorophenylmethylidene, 2,4-difluorophenylmethylidene, 2,4,6-trichlorophenylmethylidene, 2,3,5-trifluorophenylmethylidene, and 2-fluorophenylmethylidene .

Examples of phenyl lower alkoxycarbonyl groups include phenylalkoxycarbonyl groups wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group such as benzyloxycarbonyl, 2-phenylethoxycarbonyl, 1-phenylethoxycarbonyl, 3-phenylpropoxycarbonyl, 4-phenylbutoxycarbonyl, 5-phenyloxycarbonyl bonyl, 6-phenylhexyloxycarbonyl, 1,1-dimethyl-2-phenylethoxycarbonyl, and 2-methyl-3-phenylpropoxycarbonyl. Examples of optionally substituted pyridyl groups on the ring

pyridine with one or more members selected from the group consisting of a cyano group and lower alkyl groups include;

optionally substituted pyridyl groups on the pyridine ring having one to three members selected from the group consisting of a cyano group and the linear and branched C1-4 alkyl groups described above;

such as (2-, 3-, or 4-) pyridyl, 2-methyl- (3-, 4-, 5-, or 6-) pyridyl, 3-methyl- (2-, 4-, 5-, or 6-) pyridyl, 4-methyl- (2- or 3-) pyridyl, 2-cyano- (3-, 4-, 5-, or 6-) pyridyl, 3-cyano- (2-, 4-, 5 -, or 6-) pyridyl, 4-cyano- (2- or 3-) pyridyl, 2,3-dimethyl- (4-, 5-, or 6-) pyridyl, 3,4,5-trimethyl- (2 - or 6-) pyridyl, 2,4-dicyano- (3-, 5-, or 6-) pyridyl, 2,4,5-tricyano- (3- or 6-) pyridyl, and 2-methyl-4- cyano- (3-, 5-, or 6-) pyridyl.

Examples of 1,3-dioxolanyl lower alkyl groups include 1,3-dioxolanylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group such as [(2- or 4-) 1,3-dioxolanyl] methyl , 2 - [(2- or 4-) 1,3-dioxolanyl] ethyl, 1 - [(2- or 4-) 1,3-dioxolanyl] ethyl, 3 - [(2- or 4-) 1,3 -dioxolanyl] propyl, 4 - [(2- or 4-) 1,3-dioxolanyl] butyl, 1,1-dimethyl-2 - [(2- or 4-) 1,3-dioxolanyl] ethyl, 5 - [(2- or 4-) 1,3-dioxolanyl] pentyl, 6 - [(2- or 4-) 1,3-dioxolanyl] hexyl, 1 - [(2- or 4-) 1,3 -dioxolanyl] isopropyl, and 2-methyl-3 - [(1-, 2-, or 4-) 1,3-dioxolanyl] propyl.

Examples of 5- to 8-membered saturated heterocyclic rings formed of R 8 and R 9 being attached together, together with the nitrogen atom to which they are attached, the heterocyclic ring optionally containing one or more additional heteroatoms, include:

5-8 membered saturated heterocyclic rings formed of R8 and R9 being bonded together, together with the nitrogen atom to which they are attached, the heterocyclic ring optionally containing one or more additional heteroatoms selected from oxygen, nitrogen and sulfur atom ;

such as pyrrolidine, piperazine, piperidine, morpholine, thiomorpholine, imidazolidine, thiazolidine, isothiazolidine, oxazolidine, isoxazolidine, isothiazolidine, pyrazolidine, perhydroazepine, and perhydroazocine. Examples of octahydropyrrolo [1,2-a] pyrazinyl groups optionally

substituted on the pyrazine ring with one or more lower alkyl groups included in octahydropyrrolo [1,2-a] pyrazinyl groups optionally substituted on the pyrazine ring with one to three straight and / or branched C 1-6 alkyl groups.

Examples of 8-azabicyclo [3,2,1] octyl groups optionally substituted on 8-azabicyclo [3,2,1] octyl groups with one or more phenoxy groups, each phenoxy substituent being optionally substituted on the phenyl ring with one or more halogen atoms include 8-azabicyclo [3,2,1] octyl groups optionally substituted on 8-azabicyclo [3,2,1] octyl group having one to three phenoxy groups, each phenoxy substituent being optionally substituted on the phenyl ring with one to three halogen atoms.

Examples of saturated 5- or 6-membered heterocyclic rings formed of R 11 and R 12, or R 13 and R 14 being attached together, together with the nitrogen atom to which they are attached, the heterocyclic ring optionally containing one or more additional heteroatoms, include : 5- or 6-membered saturated heterocyclic rings formed of

R 11 and R 12, or R 13 and R 14 being attached together, together with the nitrogen atom to which they are attached, the heterocyclic ring optionally containing one or more additional heteroatoms selected from oxygen, nitrogen and sulfur;

such as pyrrolidine, piperazine, piperidine, morpholine, thiomorpholine, imidazolidine, thiazolidine, isothiazolidine, oxazolidine, isoxazolidine, isothiazolidine, and pyrazolidine.

Examples of phenyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; lower alkylthio groups; lower alkoxy groups optionally substituted with one or more halogen atoms; halogen atoms; a phenyl group; lower alkylammonium groups; a cyan group; a phenoxy group; cycloalkyl groups; pyrrolidinyl groups optionally substituted with one or more oxo groups; 1,2,3,4-tetrahydroisoquinolylcarbonyl groups; 1,2,3,4-tetrahydroquinolylcarbonyl groups optionally substituted by one or more lower alkyl groups; 1,2,3,4-tetrahydroquinoxalinylcarbonyl groups optionally substituted by one or more lower alkyl groups; thiazole groups optionally substituted with one or more phenyl groups; a carbamoyl group; phenyl lower alkoxy groups; lower alkylsulfonylamino groups; anilino groups optionally substituted with one or more halogen atoms; phenyl lower alkyl groups; hydroxy-substituted lower alkyl groups include:

optionally substituted phenyl groups on the phenyl ring having one to three members selected from the group consisting of linear and branched C-ι-β alkyl groups optionally substituted with one to three halogen atoms; straight and branched C1-6 alkylthio groups; C1-6 straight and branched alkoxy groups optionally substituted with one to three halogen atoms; halogen atoms; a phenyl group; amino groups optionally substituted with one or two straight and / or branched C1-6 alkyl groups; a cyan group; a phenoxy group; C3.8 cycloalkyl groups; pyrrolidinyl groups optionally substituted with one or two oxo groups; 1,2,3,4-tetrahydroisoquinolylcarbonyl groups; 1,2,3,4-tetrahydroquinolylcarbonyl groups optionally substituted with one to three straight and / or branched C 1-6 alkyl groups; 1,2,3,4-tetrahydroquinoxalinylcarbonyl groups optionally substituted with one to three straight and / or branched C1-6 alkyl groups; thiazolyl groups optionally substituted with one to three phenyl groups; a carbamoyl group; phenyl alkoxy groups wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group; straight and branched C1-6 alkylsulfonylamino groups; anilino groups optionally substituted with one to three halogen atoms; phenyl alkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group; and hydroxy substituted alkyl groups wherein the alkyl moiety is a straight or branched C1-4 alkyl group substituted with one to three hydroxy groups;

such as (2-, 3-, or 4-) trifluoromethylphenyl, (2-, 3-, or 4-) methylthio-phenyl, (2-, 3-, or 4-) trifluoromethoxyphenyl, (2-, 3-, or 4-) ethylphenyl, (2-, 3-, or A-) propylphenyl, (2-, 3-, or 4-) butylphenyl, (2-, 3-, or 4-) pentylphenyl, (2-, 3 -, or 4-) hexylphenyl, (2-, 3-, or 4-) isopropylphenyl, (2-, 3-, or 4-) chlorophenyl, (2-, 3-, or 4-) fluorophenyl, (2- , 3-, or 4-) phenylphenyl, (2-, 3-, or 4-) dimethylaminophenyl, (2-, 3-, or 4-) cyanophenyl, (2-, 3-, or 4-) phenyloxyphenyl, ( 3,4-, 2,3-, 2,6-, or 3,5-) dimethylphenyl, (3,4-, 2,3-, 2,6-, or 3,5-) difluorophenyl, 2-chloro -4-methylphenyl, (2-,

3-, or 4-) cyclohexylphenyl, (2-, 3-, or 4-) benzyloxyphenyl, (2-, 3-, or 4-) methylsulfonylaminophenyl, (2-, 3- or 4-) anilinophenyl, ( 3,4-, 2,3-, 2,6- or 3,5-) dimethoxy-

phenyl, 3-chloro-4-methoxyphenyl, 3-chloro-4-methylphenyl, 3-methoxy-5-trifluoromethylphenyl, 2-chloro-5-trifluoromethylphenyl, 2-chloro-6-cyanophenyl, 2-chloro-5- carbamylphenyl, (2-, 3-, or 4-) phenylmethylphenyl, (2-, 3-, or 4-) pyrrolidinylphenyl, (2-, 3-, or A-) [(1-, 2-, 3 -, or 4-) (1,2,3,4-tetrahydroisoquinolylcarbonyl)] phenyl, (2-, 3-, or

4-) [(1-, 2-, 3-, or 4-) (6-methyl-1,2,3,4-tetrahydroquinolylcarbonyl)] phenyl, (2-, 3-, or 4-) (4- fluoroanilino) phenyl, (2-, 3- or 4-) [4-methyl-1- (1,2,3,4-tetrahydro-

quinoxalinyl) carbonyl] phenyl, and (2-, 3-, or 4-) [(4- or 5-) phenylthiazolyl-2-yl] phenyl.

Examples of optionally substituted lower alkyl phenyl groups on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; lower alkoxy groups optionally substituted with one or more halogen atoms; halogen atoms; and a phenyl group include: phenyl alkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the phenyl ring with one to three members selected from the group consisting of C1-6 alkyl groups. and branched optionally substituted with one to three halogen atoms; straight and branched C1-6 alkoxy groups optionally substituted with one to three halogen atoms; halogen atoms; and a phenyl group;

such as benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenylhexyl, 2-methyl-3-phenylpropyl, 1,1-methylphenyl. dimethyl-2-phenylethyl, 1,1-diphenylmethyl, 2,2-diphenylethyl, 3,3-diphenylpropyl, 1,2-diphenylethyl, 4-chlorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 3-fluorobenzyl, 4-fluorobenzyl, (2- or 4-) Bromobenzyl, 2,3-dichlorobenzyl, 2,4-dichlorobenzyl, 3-chloro-4-fluorobenzyl, 2,4,6-trifluorobenzyl, 3-trifluoromethylbenzyl, 4-trifluoromethylbenzyl, 2-methylbenzyl , 3-methylbenzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 2,4-dimethylbenzyl, 2,4,6-trimethylbenzyl, 2-phenylbenzyl, 3-phenylbenzyl, 4-phenylbenzyl, 2,4-diphenylbenzyl 2,4,6-triphenylbenzyl,

2-trifluoromethoxybenzyl, 3-trifluoromethoxybenzyl, 4-trifluoromethoxybenzyl, 3-chloro-4-difluoromethoxybenzyl, 4-chloro-3-trifluoromethylbenzyl, 2-methoxybenzyl,

3-methoxybenzyl, 4-methoxybenzyl, 3,4-dimethoxybenzyl, 3,4,5-trimethoxybenzyl, 2- (4-methoxyphenyl) ethyl, 2- (2-methoxyphenyl) ethyl, and 2- (4-chlorophenyl) ethyl.

Examples of lower alkyl substituted lower alkyl amino groups include:

Aminoalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group having in the amino group one or two straight and / or branched C 1-6 alkyl groups;

such as / N-methylaminomethyl, N / N-diethylaminomethyl, N / N-di-propylaminoethyl, N / N-diisopropylaminoethyl, 3- (N / N-dimethylamino) propyl, 4- (Î ±, β-dimethylamino) butyl, 5- (Î ±, Î ± -dimethylamino) pentyl, and 6- (Î ±, Î ± -dimethylamino) hexyl.

Examples of optionally substituted lower alkyl pyrazinyl groups

The pyrazine ring having one or more lower alkyl groups include:

Pyrazinylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the pyrazine ring with one to three straight and / or branched C 1-6 alkyl groups;

such as (2- or 3-) pyrazinylmethyl, (1- or 2-) (2- or 3-pyrazinyl) ethyl, 3- (2- or 3-) pyrazinylpropyl, 4- (2- or 3-) pyrazinylabutyl, 5- (2- or 3-) pyrazinylpentyl, 6- (2- or 3-) pyrazinylhexyl, 2-methyl-5-pyrazinylmethyl, (1- or 2-) (2-methyl-5-pyrazinyl) ethyl, 3- (2-methyl-5-pyrazinyl) propyl, 4- (2-ethyl-5-pyrazinyl) butyl, 5- (2-ethyl-5-pyrazinyl) pentyl, and 6- (2-methyl-5-pyrazinyl) ) hexyl.

Examples of pyrazolyl lower alkyl groups optionally substituted on the pyrazoline ring with one or more lower alkyl groups include: Pyrazolylalkyl groups wherein the alkyl moiety is a C1-6 group

straight or branched alkyl optionally substituted on the pyrazoline ring with one to three straight and / or branched C1-6 alkyl groups;

such as (3-, 4-, or 5-) pyrazolylmethyl, (1- or 2-) (3-, 4-, or 5-) pyrazolylethyl, 3- (3-, 4-, or 5-) pyrazolylpropyl, 4- (3-, 4-, or 5-) pyrazolylbutyl, 5- (3-, 4-, or 5-) pyrazolylpentyl, 6- (3-, 4-, or 5-) pyrazolylhexyl, [1-methyl- (3-, 4-, or 5-) pyrazolyl] methyl, [1,5-dimethyl- (3- or 4-) pyrazolyl] methyl, and [1,5-dimethyl- (3- or 4-) pyrazolyljetyl.

Examples of piperidinyl groups optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl group; a benzoyl group; and optionally substituted lower alkyl phenyl groups on the phenyl ring having one or more selected halogen atom members and lower alkyl groups include:

optionally substituted piperidinyl groups on the piperidine ring having one to three members selected from the group consisting of straight and branched C 1-6 alkyl groups; a benzoyl group; and lower alkyl phenyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group, optionally substituted on the phenyl ring with one to three members selected from the group consisting of halogen atoms and linear C1-6 alkyl groups and branched;

such as N-methyl- (2-, 3-, or 4-) piperidinyl, N-methyl- (2-, 3-, or 4-)

piperidinyl, Nn-propyl- (2-, 3-, or 4-) piperidinyl, N-benzoyl- (2-, 3-, or 4-) piperidinyl, 1-benzyl-4-piperidinyl, 1-phenylethyl -4-piperidinyl, 1- (2-, 3-, or 4-) chlorophenylmethyl-4-piperidinyl, and 1- (2-, 3-, or 4-) methylphenylmethyl-4-piperidinyl, 1,2, 3-trimethyl- (4-, 5-, or 6-) piperidinyl, 1-benzyl-3-methyl- (2-, 4-, 5-, or 6-) piperidinyl, and 1-benzoyl-2- benzyl- (3-, 4-, 5-, or 6-) piperidinyl.

Examples of 3,4-dihydrocarbostyryl groups optionally substituted with one or more lower alkyl groups include 3,4-dihydrocarbostyryl groups optionally substituted with one to three straight and / or branched C 1-6 alkyl groups, such as 3,4 -dihydro- (5-, 6-, 7-, or 8-) carbosyryl and (6-, 7-, or 8-) methyl-3,4-dihydro-5-carbostyril.

Examples of quinolyl groups optionally substituted with one or more lower alkyl groups include optionally substituted quinolyl groups having one to three straight and / or branched C1-6 alkyl groups, such as (2-, 3-, 4-, 5-, 6-, 7- or 8-) quinolyl and 2-methyl-4-quinolyl.

Examples of carbazolyl groups optionally substituted with one or more lower alkyl groups include carbazolyl groups optionally substituted with one to three straight and branched C1-6 alkyl groups, such as V-methyl- (2-, 3-, 4-, or 5-methyl). -) carbazolyl and / V-ethyl- (2-, 3-, 4-, or 5-) carbazolyl.

Examples of lower alkyl lower alkylcarbamoyl phenyl groups include phenylalkylcarbamoylalkyl groups wherein each of the two moieties is a straight or branched C1-6 alkyl group such as phenylmethylcarbamoylmethyl, (1- or 2-) phenylethyl carbamoylmethyl, (1- or 2-) phenylethylcarbamethylethyl, 3- (2-phenylethylcarbamoyl) propyl, 4- (2-phenylethylcarbamoyl) butyl, 5- (2-phenylethylcarbamoyl) pentyl, and 6- (2-phenylethylcarbamoyl) hexyl.

Examples of phenylcarbamoyl lower alkyl groups include phenylcarbamoylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as phenylcarbamoylmethyl, (1- or 2-) phenylcarbamoylethyl, 3- (phenylcarbamoyl) propyl, 4 - (phenylcarbamoyl) butyl, 5- (phenylcarbamoyl) pentyl, and 6- (phenylcarbamoyl) hexyl.

Examples of phenyl ring optionally substituted anilino groups having one or more lower alkoxy groups, each lower alkoxy substituent being substituted with one or more halogen atoms, include:

optionally substituted anilino groups on the phenyl ring having one to three straight and / or branched C 1-6 alkoxy groups, each alkoxy substituent optionally being substituted with one to three halogen atoms;

such as (2-, 3-, or 4-) chloromethoxyanilino, and (2-, 3-, or 4-) trifluoromethoxyanilino.

Examples of amino groups substituted on the amino group with

one or more lower alkyl groups and also substituted on the phenyl ring with one or more halogen atoms include:

amino-substituted anilino groups having one to three straight and / or branched C1-6 alkyl groups and also substituted on the phenyl ring having one to three halogen atoms;

such as N-methyl- (2-, 3-, or 4-) chloroanilino, N-ethyl- (2-, 3-, or 4-) chloroanilino, N-methyl- (2-, 3-, or 4-) bromoanilino, N-methyl- (2-, 3-, or 4-) fluoroanilino, N-ethyl- (2-, 3-, or 4-) iodoanilino, and / Vn -propyl- (2). -, 3-, or 4-) chloroaniline.

Examples of 5- and 6-membered unsaturated heterocyclic rings

R 8 and R 9 being attached together, together with the nitrogen atom to which they are attached, include (2- or 3-) pyrroline, 1,2-dihydropyridine, 2,3-dihydropyridine, 1,2,3 , 4-tetrahydropyridine, and 1,2,5,6-tetrahydropyridine.

Examples of optionally substituted benzoyl groups on the phenyl ring having one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms; a phenyl group; halogen atoms; a cyan group; a phenoxy group; lower alkoxycarbonyl groups; pyrazolyl groups; and lower alkoxy groups optionally substituted with one or more halogen atoms include:

optionally substituted benzoyl groups on the phenyl ring having one to three members selected from the group consisting of the linear and branched C1-6 alkyl groups described above optionally substituted with one to three halogen atoms; a phenyl group; halogen atoms; a cyan group; a phenoxy group; the linear and branched C1-6 alkoxycarbonyl groups described above; pyrazolyl groups; and the linear and branched C1-6 alkoxy groups described above optionally substituted with one to three halogen atoms;

such as benzoyl, 4-methylbenzoyl, 3-methylbenzoyl, 2-methylbenzoyl, 4-tert-butylbenzoyl, 2,4-dimethylbenzoyl, 2,4,6-trimethylbenzoyl, 3-trifluoromethylbenzoyl, 4-trifluoromethylbenzoyl, 2- trifluoromethylbenzoyl, 4-phenylbenzoyl, 4-chlorobenzoyl, 3-chlorobenzoyl, 2-chlorobenzoyl, 4-fluorobenzoyl, 3-fluorobenzoyl, 2-fluorobenzoyl, 2-bromobenzoyl, 4-bromobenzoyl, 3,4-dibenzoyl, 2,3-dichlorobenzoyl, 2-chloro-4-fluorobenzoyl, 2-methoxy-5-chlorobenzoyl, 4-methoxybenzoyl, 3-methoxybenzoyl, 2-methoxybenzoyl, 3,4-dimethoxybenzoyl, 3,4,5-trimethoxybenzoyl, 3-trifluoromethoxybenzoyl, 4-trifluoromethoxybenzoyl, 2-trifluoromethoxybenzoyl, 3-cyano-benzoyl, 4-cyanobenzoyl, 2-cyanobenzoyl, 2-phenoxybenzoylcarbonylbenzoyl, 4-phenoxybenzoylcarbonyl 2-tert-butoxycarbonylbenzoyl, and 4- (1-pyrazolyl) benzoyl.

Examples of alkanoyl groups include straight and branched C-1 alkanoyl groups, such as, in addition to the above described lower alkanoyl, heptanoyl, octanoyl, nonanoyl, decanoyl, and 2-ethylhexanoyl groups.

Examples of phenyl lower alkanoyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups include: phenyl alkanoyl groups wherein the alkanoyl moiety is a group

Straight or branched C 2-6 alkanoyl, optionally substituted on the phenyl ring with one to three members selected from the group consisting of halogen atoms and straight and branched C 1-6 alkyl groups;

such as 2-phenylacetyl, 3-phenylpropionyl, 2-phenylpropionyl, 4-phenylbutyryl, 5-phenylpentanoyl, 6-phenylhexanoyl, 2,2-dimethyl-3-phenylpropionyl,

2-methyl-3-phenylpropionyl, 2- (4-fluorophenyl) acetyl, 3- (2,5-difluorophenyl) propionyl, 2- (2,4-difluorophenyl) propionyl, 4- (3,4-difluorophenyl) butyryl, 5- (3,5-difluorophenyl) pentanoyl, 6- (2,6-difluorophenyl) hexanoyl, 2- (2-chlorophenyl) acetyl,

3- (3-chlorophenyl) propionyl, 2- (4-chlorophenyl) propionyl, 4- (2,3-dichlorophenyl) propionyl, 5- (2,4-dichlorophenyl) pentanoyl, 6- (2,5-dichlorophenyl ) hexanoyl, 2- (3,4-

dichlorophenyl) acetyl, 3- (2,6-dichlorophenyl) propionyl, 2- (3-fluorophenyl) propionyl,

4- (2-fluorophenyl) butyryl, 5- (3-bromophenyl) pentanoyl, 6- (4-iodophenyl) hexanoyl, 2- (2-bromophenyl) acetyl, 3- (4-bromophenyl) propionyl, 2- (3, 5-dichlorophenyl) propionyl, 4- (2,4,6-trifluorophenyl) butyryl, 5- (3,4-difluorophenyl) pentanoyl, 6- (2-iodophenyl) hexanoyl, 2- (3-iodophenyl) acetyl, 3- (4-iodophenyl) propionyl, 2- (2,3-dibromophenyl) propionyl, 4- (2,4-diiodophenyl) butyryl, 2- (2,4,6-trichlorophenyl) acetyl

1a, 2- (4-methylphenyl) acetyl, 3- (2,5-dimethylphenyl) propionyl, 2- (2,4-diethylphenyl) propionyl, 4- (3,4-di-n-propylphenyl) butyryl, 2- (2-ethylphenyl) acetyl, 3- (3-n-propylphenyl) propionyl, 2- (4-t-t-butylphenyl) propionyl, 2- (2,4,6-trimethylphenyl) acetyl, 2- (2 , 5-dichloro-4-methylphenyl) acetyl, 2- (3-methyl-4-chlorophenyl) acetyl, 4- (2-n-butylphenyl) butyryl, 5- (3-n-pentylphenyl) pentanoyl, and 6- ( 4-n-hexylphenyl) hexanoyl. Examples of optionally lower alkanoyl phenoxy groups

Substituted in the phenyl ring with one or more halogen atoms include:

Phenoxy alkanoyl groups wherein the alkanoyl moiety is a straight or branched C 2-6 alkanoyl group, optionally substituted on the phenyl ring with one to three halogen atoms; Such as in addition to the above described phenoxy alkanoyl groups include

ferior, 2- (4-chlorophenoxy) acetyl, 2- (4-fluorophenoxy) acetyl, 3- (2,5-difluorophenoxy) propionyl, 2- (2,4-difluorophenoxy) propionyl, 4- (3,4 -difluorophenoxy) butyryl, 5- (3,5-difluorophenoxy) pentanoyl, 6- (2,6-difluorophenoxy) hexanoyl, 2- (2-chlorophenoxy) acetyl, 3- (3-chlorophenoxy) propionyl, 2- ( 4-chlorophenoxy) propionyl, 4- (2,3-dichlorophenoxy) propionyl, 5- (2,4-dichlorophenoxy) pentanoyl, 6- (2,5-dichlorophenoxy) hexanoyl, 2- (3,4-dichlorophenoxy) acetyl, 3- (2,6-dichlorophenoxy) propionyl, 2- (3-fluorophenoxy) propionyl, 4- (2-fluorophenoxy) butyryl, 5- (3-bromophenoxy) pentanoyl, 6- (4-iodophenoxy) hexanoyl, 2 - (2-bromophenoxy) acetyl,

3- (4-bromophenoxy) propionyl, 2- (3,5-dichlorophenoxy) propionyl, 4- (2,4,6-trifluorophenoxy) butyryl, 5- (3,4-difluorophenoxy) pentanoyl, 6- (2-iodophenoxy ) hexanoyl, 2- (3-iodophenoxy) acetyl, 3- (4-iodophenoxy) propionyl, 2- (2,3-dibromophenoxy) propionyl, 4- (2,4-diiodophenoxy) butyryl, and 2- (2,4,6-trichlorophenoxy) acetyl.

Examples of phenyl lower alkenylcarbonyl groups include phenylalkenylcarbonyl groups containing one to three double bonds wherein the alkenyl moiety is a straight or branched C 2-6 alkenyl group such as styrylcarbonyl (trivial name: cinnamoyl), 3-phenyl-2-propenylcarbonyl , 4-phenyl-2-butenylcarbonyl, 4-phenyl-3-butenylcarbonyl, 5-phenyl-4-pentenylcarbonyl, 5-phenyl-3-pentenylcarbonyl, 6-phenyl-5-hexenylcarbonyl, 6-phenyl-4-hexenylcarbonyl, 6 phenyl-3-hexenylcarbonyl, 4-phenyl-1,3-butadienylcarbonyl, and 6-phenyl-1,3,5-hexahytrienylcarbonyl.

Examples of optionally substituted pyridylcarbonyl groups

on the pyridine ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more halogen atoms, include: optionally substituted pyridylcarbonyl groups on the pyridine ring

one with one to three members selected from the group consisting of halogen atoms and the linear and branched C1-6 alkyl groups described above optionally substituted with one to three halogen atoms;

such as (2-, 3-, or 4-) pyridylcarbonyl, 2-chloro- (3-, 4-, 5-, or 6-) pyridylcarbonyl, 2,6-dichloro- (3-, 4-, or 5) -) pyridylcarbonyl, 2,3-dichloro- (4-, 5-, or 6-) pyridylcarbonyl, 2-trifluoromethyl- (3-, 4-, 5-, or 6-) pyridylcarbonyl, 2-bromo- (3- , 4-, 5-, or 6-) pyridylcarbonyl, 2,6-difluoro- (3-, 4-, or 5-) pyridylcarbonyl, 4-methyl- (2-, 3-, 5-, or 6 -) pyridylcarbonyl, 3-chloro- (2-, 4-, 5-, or 6-) pyridylcarbonyl, 2,5-dibromo- (3-, 4-, or 5-) pyridylcarbonyl, 2-ethyl-4 -chloro- (3-, 5-, or 6-) pyridylcarbonyl, 2,4,6-trifluoro- (3- or 5-) pyridylcarbonyl, 2,4-dimethyl- (3-,

5-, or 6-) pyridylcarbonyl, 2,4,6-trimethyl- (3- or 5-) pyridylcarbonyl, and 2-methyl-4-chloro- (3-, 5-, or 6-) pyridylcarbonyl.

Examples of piperidinylcarbonyl groups optionally substituted on the piperidine ring with one or more lower alkanoyl groups include piperidinylcarbonyl groups optionally substituted on the piperidine ring with one to three straight and / or branched C1-6 alkanoyl groups such as (2-, 3-, or 4-) piperidinylcarbonyl, 1-acetyl- (2-, 3-, or 4-) piperidinylcarbonyl, 1-n-propanoyl- (2-, 3-, or 4-) piperidinylcarbonyl, 1-isopropanoyl- (2-, 3-, or 4-) piperidinylcarbonyl, 1-β-butyryl- (2-, 3-, or 4-) piperidinylcarbonyl, 1-7-pentanoyl (2-, 3-, or 4-) piperidinylcarbonyl 1-1-hexanoyl- (2-, 3-, or 4-) piperidinylcarbonyl, 1,2-diacetyl- (3-, 4-, 5-, or 6-) piperidinylcarbonyl, 1,2,3 -triacetyl- (4-, 5-, or

6-) piperidinylcarbonyl, 2-acetyl- (1-, 3-, 4-, 5-, or 6-) piperidinylcarbonyl, 3-propanoyl- (1-, 2-, 4-, 5-, or 6-) piperidinylcarbonyl , and 2-formyl-4-propanoyl- (1-, 3-, 5-, or 6-) piperidinylcarbonyl.

Examples of tetrahydropyranylcarbonyl groups include 2-tetrahydropyranylcarbonyl, 3-tetrahydropyranylcarbonyl, and 4-tetrahydropyranylcarbonyl.

Examples of optionally substituted benzothienylcarbonyl groups

benzothiophene ring having one or more halogen atoms included in benzothienylcarbonyl groups optionally substituted on the benzothiophene ring having one to three halogen atoms, such as (2-, 3-, 4-, 5-, 6- , or 7-) benzothienylcarbonyl, [3-chloro- (2-, 4-, 5-, 6-, or 7-) benzothienylcarbonyl, [4-bromo- (2-, 3-, 5-, 6-, or 7-) benzothienylcarbonyl, [5-fluoro- (2-, 3-, 4-, 6-, or 7-) benzothienylcarbonyl, [6-iodo- (2-, 3-, 4-, 5-, or 7- ) benzothienylcarbonyl, [7-chloro- (2-, 3-, 4-, 5-, or 6-) benzothienylcarbonyl, [2-chloro- (3-, 4-, 5-, 6-, or 7-) benzothienyl ] carbonyl, [2,3-dichloro- (4-, 5-, 6-, or 7-) benzothienylcarbonyl, and [3,4,6-trichloro- (2-, 5- or 7-) benzothienyl] carbonyl. Examples of optionally substituted lower alkyl pyridyl groups

A pyridine ring having one or more members selected from the group consisting of halogen atoms and lower alkyl groups, each lower alkyl substituent optionally being substituted with one or more halogen atoms, include: Pyridylalkyl groups wherein the alkyl moiety is a C1-6 group

straight or branched alkyl optionally substituted on the one to three membered pyridine ring selected from the group consisting of halogen atoms and the above described straight and branched C1-6 alkyl groups optionally substituted with one to three halogen atoms; such as (2-, 3-, or 4-) pyridylmethyl, 2 - [(2-, 3-, or 4-) pyridyl] ethyl,

1 - [(2-, 3-, or 4-) pyridyl] ethyl, 3 - [(2-, 3-, or 4-) pyridylpropyl, 4 - [(2-, 3-, or 4-) pyridyl] butyl, 1,1-dimethyl-2 - [(2-, 3-, or 4-) pyridyl] ethyl, 5 - [(2-, 3-, or 4-) pyridyl] pentyl, 6 - [( 2-, 3-, or 4-) pyridyl] hexyl, 1 - [(2-, 3-, or 4-) pyridyl] isopropyl, 2-methyl-3 - [(2-, 3-, or 4-) pyridyl] propyl, [2-chloro- (3-, 4-, 5-, or 6-) pyridyl] methyl, [2,3-dichloro- (4-, 5-, or 6-) pyridyl] methyl, [2-bromo] (3-, 4-, 5-, or 6-) pyridylmethyl, [2,4,6-trifluoro- (3-, 5-, or 6-) pyridyl] methyl, [2-trifluoromethyl- (3-, 4 -, 5-, or 6-) pyridylmethyl, [2-methyl- (3-, 4-, 5-, or 6-) pyridylmethyl, [2-ethyl- (3-, 4-, 5-, or 6- ) pyridyl] methyl, 2- [2-n-propyl- (3-, 4-, 5-, or 6-) pyridyl] ethyl, 3- [2- / 7-butyl- (3-, 4-, 5 -, or 6-) pyridyl] propyl, 4- [2-n-pentyl- (3-, 4-, 5-, or 6-) pyridyl] butyl, 5- [2-n-hexyl- (3-, 4-, 5-, or 6-) pyridyl] pentyl, 6- [2-isopropyl- (3-, 4-, 5-, or 6-) pyridyl] hexyl, [2-tert-butyl- (3 -, 4-, 5-, or 6-) pyridyl] methyl, [2,4-dimethyl- (3-, 5-, or 6-) pyridyl] methyl, [2,4,6-trime til- (3- or 5-) pyridyl] methyl, [2,4-ditrifluoromethyl- (3-, 5-, or 6-) pyridyl] methyl, 2- (2,4-bistrifluoromethyl) - (3-,5 -, or 6-) pyridyl) ethyl, and 3- [2-methyl-6-chloro- (3-, 4-, or 5-) pyridyl] propyl.

Examples of thienyl lower alkyl groups optionally substituted on the thiophene ring with one or more halogen atoms include: Thienylalkyl groups wherein the alkyl moiety is a C 1-6 alkyl group.

straight or branched kyl, optionally substituted on the thiophene ring with one to three halogen atoms;

such as [(2- or 3-) thienyl] methyl, 2 - [(2- or 3-) thienyl] ethyl, 1 - [(2- or 3-) thienyljetyl, 3 - [(2- or 3-) thienyl] propyl, 4 - [(2- or 3-) thienyl] butyl, 5 - [(2- or 3-) thienyl] pentyl, 6 - [(2- or 3-) thienyl] hexyl, 1,1-dimethyl 2 - [(2- or 3-) thienyl] ethyl, 2-methyl-3 - [(2- or 3-) thienyl] propyl, [2-chloro- (3-, 4-, or 5-) thienyl] methyl, [4-bromo- (2-, 3-, or 5-) thienyl] methyl, [5-fluoro- (2-, 3-, or 4-) thienyl] methyl, [3-iodo- (2- , 4-, or 5-) thienyl] methyl, [2,3-dichloro- (4- or 5-) thienyl] methyl, (2,4,5-trichloro-3-thienyl) methyl, 2- [2- fluoro- (3-, 4-, or 5-) thienyljetyl, 1- [4-iodo- (2-, 3-, or 5-) thienyl] ethyl, 3- [3-chloro- (2-, 4- , or 5-) thienyl] propyl, 4- [4,5-dichloro- (2- or 3-) thienyl] butyl, 5- (2,4,5-trichloro-3-thienyl) pentyl, and 6- [2- chloro- (3-, 4-, or 5-) thienyl] hexyl.

Examples of amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups include: amino groups optionally substituted with one or two members.

arms selected from the group consisting of linear and branched C1-6 alkyl groups and linear and branched C1-6 alkanoyl groups;

such as amino, formylamino, acetylamino, propionylamino, butyrylamino, isobutyrylamino, pentanoylamino, tert-butylcarbonylamino, hexanoylamino, N, Î ± -diacetylamino, V-acetyl-β-propionylamino, methylamino, ethylamino, n-amino propylamino, isopropylamino, n-butylamino, n-pentylamino, n-hexylamino, dimethylamino, 3-diethylamino, diisopropylamino, N-methyl-Î ± -n-propylamino, N-meXW-Nn-hexylamino, A / methyl - / V-acetylamino, and A / -ethyl- / V-acetylamino.

Examples of optionally substituted lower alkyl phenyl groups on the phenyl ring with one or more members selected from the group consisting of lower alkoxy groups optionally substituted with one or more halogen atoms; a cyan group; lower alkyl groups optionally substituted with one or more halogen atoms; amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups; halogen atoms; lower alkoxycarbonyl groups; lower alkanoyloxy groups; lower alkylsulfonyl groups; lower alkylthio groups; and pyrrolidinyl groups include:

Mono- and di-phenylalkyl groups wherein the alkyl moiety is a linear or branched C1-6 alkyl group, optionally substituted on the phenyl ring with one to three members selected from the group consisting of the linear and branched C1-6 alkoxy groups described above optionally substituted with one to three halogen atoms; a cyan group; the linear and branched C1-6 alkyl groups described above optionally substituted with one to three halogen atoms; optionally substituted amino groups described above with one or two members selected from the group consisting of straight and branched C1-6 alkyl groups and straight and branched C1-6 alkanoyl groups; halogen atoms; the linear and branched C1-6 alkoxycarbonyl groups described above; the linear and branched C 2-6 alkanoyloxy groups described above; the linear and branched C1-6 alkylsulfonyl groups described above; the linear and branched C1-6 alkylthio groups described above; and pyrrolidinyl groups;

such as benzyl, 1-phenylethyl, 2-phenylethyl, 3-phenylpropyl, 2-phenylpropyl, 4-phenylbutyl, 5-phenylpentyl, 4-phenylpentyl, 6-phenylhexyl, 2-methyl-3-phenylpropyl, 1, 1-dimethyl-2-phenylethyl, 1,1-diphenylmethyl, 2,2-diphenylethyl, 3,3-diphenylpropyl, 1,2-diphenylethyl, 4-chlorobenzyl, 2-chlorobenzyl, 3-chlorobenzyl, 3-fluorobenzyl, 4-fluorobenzyl, 2-fluorobenzyl, 4-bromobenzyl, 3-bromobenzyl, 2-bromobenzyl, 1- (2-chlorophenyl) ethyl, 2,3-dichlorobenzyl, 2,4,6-trifluorobenzyl, 2-trifluoromethylbenzyl , 3-Trifluoromethylbenzyl, 4-trifluoromethylbenzyl, 2-methylbenzyl, 3-methylbenzyl, 4-methylbenzyl, 4-tert-butylbenzyl, 4-n-butylbenzyl, 2,4-dimethylbenzyl, 2,4,6-trimethylbenzyl, 2 -phenylbenzyl, 4-phenylbenzyl, 2,4-diphenylbenzyl, 2,4,6-triphenylbenzyl, 2-trifluoromethoxybenzyl, 3-trifluoromethoxybenzyl, 4-trifluoromethoxybenzyl, 4-difluoromethoxybenzyl, 2-methoxybenzyl, 3-methoxybenzyl , 4 - [α-butoxybenzyl, 4-tert-butoxybenzyl, 1- (3-methoxyphenyl) ethyl, 1- (4-methoxyphenyl) ethyl, 1- (2-methoxyphenyl) ethyl, 3,4-dimethoxybenzyl, 3,4,5-trimethoxybenzyl, 4-methoxycarbonylbenzyl, 3-ethoxycarbonylbenzyl, 2-7-propoxycarbonylbenzyl, 2,4 dimethoxycarbonylbenzyl, 2,4,6-trimethoxycarbonylbenzyl, 1- (4-n-butoxyphenyl) ethyl, 4-tert-butoxycarbonylbenzyl, 4-methylthiobenzyl, 3-methylthiobenzyl, 2-methylthiobenzyl, 4-ethylthiobenzyl, 2,4- dimethylthiobenzyl, 2,4,6-trimethylthiobenzyl, 4-methylsulfonylbenzyl, 3-methylsulfonylbenzyl, 2-methylsulfonylbenzyl, 3,4-dimethylsulfonylbenzyl, 3,4,5-trimethylsulfonylbenzyl, 4-methoxy-3-chlorobenzyl, 4- (V-acetylamino) benzyl, 4- (N, N-diethylamino) benzyl, 4- (V-V-dimethylamino) benzyl, 4- (N-methylamino) benzyl, 3-aminobenzyl, 2-aminobenzyl , 4-Aminobenzyl, 4-acetyloxybenzyl, 2,3-diaminobenzyl, 3,4,5-triaminobenzyl, 4-methyl-3-fluorobenzyl, 4-cyanobenzyl, 3-cyanobenzyl, 2-cyanobenzyl, 4- (1-pyrrolidinyl) benzyl, 4-methoxy-2-chloro-benzyl, and 3-chloro-5-methylbenzyl.

Examples of thiazolyl lower alkyl groups include thiazolylalkyl groups wherein the alkyl moiety is a straight or branched C1-6 alkyl group such as [(2-, 4-, or 5-) thiazolyl] methyl, 2 - [(2 -, 4-, or 5-) thiazolyl] ethyl, 1 - [(2-, 4-, or 5-) thiazolyl] ethyl, 3 - [(2-, 4-, or 5-) thiazolyl] propyl, 4 - [(2-, 4-, or 5-) thiazoylbutylal 5 - [(2-, 4-, or 5-) thiazolyl] pentyl, 6 - [(2-, 4-, or 5-) thiazolylhexyl, 1,1-dimethyl-2 - [(2-, 4-, or 5-) thiazolyl] ethyl, and [2-methyl-3 - [(2-, 4-, or 5-) thiazolyl] propyl.

Examples of imidazolyl lower alkyl groups optionally substituted on the imidazole ring with one or more lower alkyl groups included:

Imidazolylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the imidazole ring with one to three linear and branched C 1-6 alkyl groups described above; such as [(1-, 2-, 4-, or 5-) imidazolyl] methyl, 2 - [(1-, 2-, 4-, or 5-)

imidazolyljetyl, 1 - [(1-, 2-, 4-, or 5-) imidazolyl] ethyl, 3 - [(1-, 2-, 4-, or 5-) imidazolyl] propyl, 4 - [( 1-, 2-, 4-, or 5-) imidazolyl] butyl, 1,1-dimethyl-2 - [(1-, 2-, 4-, or 5-) imidazolyl] ethyl, 5 - [(1- , 2-, 4-, or 5-) imidazolyl] pentyl, 6 - [(1-, 2-, 4-, or 5-) imidazolyl] hexyl, 1 - [(1-, 2-, 4-, or 5-) imidazolyl] isopropyl, 2-methyl-3 - [(1-, 2-, 4-, or 5-) imidazolyl] propyl, [1-methyl- (2-, 4-, or 5-) imidazolyl] methyl, [1-ethyl- (2-, 4-, or 5-) imidazolyl] methyl, [1-n-propyl- (2-, 4-, or 5-) imidazolyl] methyl, [1- [1- butyl- (2-, 4-, or 5-) imidazolyl] methyl, [1-n-pentyl- (2-, 4-, or 5-) imidazolyl] methyl, [1- n -hexyl- (2-, 4-, or 5-) imidazolyl] methyl, 2- [2-methyl- (1-, 4-, or 5-) imidazolyl] ethyl, 1- [1-ethyl- (2-, 4-, or 5- ) imidazolyljetyl, 3- [1-ethyl- (2-, 4-, or 5-) imidazolyl] methyl, 4- [1-n-propyl- (2-, 4-, or 5-) imidazolyl] butyl, 5 - [1-n-butyl- (2-, 4-, or 5-) imidazolyl] pentyl, 6- [1-n-pentyl- (2-, 4-, or 5-) imidazolyl] hexyl, [ 1,2-dimethyl- (4- or 5-) imidazolyl] methyl, and (1,2,4-t Rimethyl-5-imidazolyl) methyl.

Examples of pyrrolyl lower alkyl groups optionally substituted on the pyrrol ring with one or more lower alkyl groups include:

Pyrrolylalkyl groups wherein the alkyl moiety is a straight or branched C 1-6 alkyl group, optionally substituted on the pyrrol ring with one to three straight and branched C 1-6 alkyl groups described above;

such as [(1-, 2-, or 3-) pyrrolyl] methyl, 2 - [(1-, 2-, or 3-) pyrrolyl] ethyl, 1 - [(1-, 2-, or 3 -) pyrrolyl] ethyl, 3 - [(1-, 2-, or 3-) pyrrolyl] propyl, 4 - [(1-, 2-, or 3-) pyrrolyl] butyl, 1,1-dimethyl-2- [(1-, 2-, or 3-) pyrrolyljetyl, 5 - [(1-, 2-, or 3-) pyrrolyl] pentyl, 6 - [(1-, 2-, or 3-) pyrrolyl] hexyl, 1 - [(1-, 2-, or 3-) pyrrolidylisopropyl, 2-methyl-3 - [(1-, 2-, or 3-) pyrrolyl] propyl, [1-methyl- (2- or 3-) pyrrophyl] methyl, [1-ethyl- (2- or 3-) pyrrolylmethyl, [1-r'-propyl- (2- or 3-) pyrrolyl] methyl, [1- A7-butyl- (2- or 3-) pyrrolylmethyl, [1-n-pentyl- (2- or 3-) pyrrolylmethyl, [1-n-hexyl- (2- or 3-) pyrrolylmethyl, 2- [2-methyl- (1-, 3- , 4-, or 5-) pyrrolyljetyl, 1- [1-ethyl- (2- or 3-) pyrrolyljetyl, 3- [1-ethyl- (2- or 3-) pyrrolylmethyl, 4- [1-n-propyl - (2- or 3-) pyrrolidylbutyl, 5- [1- n -butyl- (2- or 3-) pyrrolyl] pentyl, 6- [1-n-pentyl- (2- or 3-) pyrrolidyl] lil] hexyl, [1,2-dimethyl- (3-, 4-, or 5-) pyrrolyl] methyl, and [1,2,4-trimethyl- (3- or 5-) pyrrolylmethyl.

Examples of lower alkyl lower alkylthio groups include alkylthioalkyl groups wherein each of the two alkyl moieties is a straight or branched C1-6 alkyl group, such as methylthiomethyl, 2-methylthioethyl, 1-ethylthioethyl, 2-ethylthioethyl, n-butylthiopropyl, 4-n-propylthiobutyl, 1,1-dimethyl-2- [α-pentylthioethyl, 5-n-hexylthiopentyl, 6-methylthiohexyl, 1-ethylthioisopropyl, and 2-methyl-3-methylthiopropyl.

Examples of phenoxycarbonyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms, lower alkyl groups, and lower alkoxy groups include:

optionally substituted phenoxycarbonyl groups on the phenyl ring having one to three members selected from the group consisting of halogen atoms, the linear and branched C1-6 alkyl groups described above, and the linear and branched C1-6 alkoxy groups described above; phenoxycarbonyl, 4-chlorophenoxycarbonyl, 3-chlorophenoxy

xicarbonyl, 2-chlorophenoxycarbonyl, 3,4-dichlorophenoxycarbonyl, 2,4,6-trichlorophenoxycarbonyl, 4-fluorophenoxycarbonyl, 3-fluorophenoxycarbonyl, 2-fluorophenoxycarbonyl, 2,4-difluorophenoxycarbonyl, 3,4,5-trifluorophenoxycarbonyl, 4-bromophenoxycarbonyl, 2-chloro-4-methoxyphenoxycarbonyl, 3-fluoro-5-methylphenoxycarbonyl, 4-methoxyphenoxycarbonyl, 3-methoxyphenoxycarbonyl, 2-methoxyphenoxycarbonyl, 3,4-dimethoxyphenoxycarbonyl, 2,4,5-trimethylcarbonyl 4-methylphenoxycarbonyl, 3-methylphenoxycarbonyl, 2-methylphenoxycarbonyl, 2,5-dimethylphenoxycarbonyl, and 2,3,4-trimethylphenoxycarbonyl.

Examples of optionally substituted phenyl lower alkoxycarbonyl groups on the phenyl ring having one or more halogen atoms include:

phenylalkoxycarbonyl groups wherein the alkoxy moiety is a straight or branched C1-6 alkoxy group, optionally substituted on the phenyl ring with one to three halogen atoms;

such as benzyloxycarbonyl, 2-phenylethoxycarbonyl, 1-phenylethoxycarbonyl, 3-phenylpropoxycarbonyl, 4-phenylbutoxycarbonyl, 5-phenylpentyloxycarbonyl, 6-phenylhexyloxycarbonyl, 1,1-dimethyl-2-phenylethoxycarbonyl, 2-methyloxy-3-phenyloxy 2-chlorobenzyloxycarbonyl, 3-chlorobenzyloxycarbonyl, 2-chlorobenzyloxycarbonyl, 3,4-dichlorobenzyloxycarbonyl, 2,4,6-trichlorobenzyloxycarbonyl, 4-fluorobenzyloxycarbonyl, 3-fluorobenzyloxycarbonyl, 2-fluoro-benzyloxycarbonyl, 2,4-difoxyl 4,5-trifluorobenzyloxycarbonyl, 4-bromobenzyloxycarbonyl, 4-nitrobenzyloxycarbonyl, and 3-nitrobenzyloxycarbonyl. Examples of quinoxalinylcarbonyl groups include 2-quinoxalinylcarbonyl, 5-quinoxalinylcarbonyl, and 6-quinoxalinylcarbonyl.

Examples of lower phenyl alkanoyl groups include phenyl alkanoyl groups wherein the alkanoyl moiety is a linear or branched C 2-6 alkanoyl group such as 2-phenylacetyl, 3-phenylpropionyl, 2-phenylpropionyl, 4-phenylbutyryl, 5-phenylpentanoyl, 6-phenylhexanoyl, 2,2-dimethyl-2-phenylpropionyl, and 2-methyl-3-phenylpropionyl.

Among the carbostyril compounds represented by General Formula (1) or salts thereof, carbostyril compounds selected from the following compounds or salts thereof are preferable:

5- [1- (biphenyl-4-ylmethyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazollidine-2,4-dione,

5- [1- (4-chlorobenzyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- [1- (4-bromobenzyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- [1- (2-naphthylmethyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- {1- [4- (heptyloxycarbonylamino) benzyl] -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione,

5- [1- (1-biphenyl-4-ylpiperidin-4-ylmethyl) -2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione,

5- {1- [1- (4-methylphenyl) piperidin-4-ylmethyl] -2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione, 5- {1- [4- (2-chlorobenzyloxycarbonylamino) benzyl] -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione,

1- (biphenyl-4-ylmethyl) -8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

8-Methoxy-1-methyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-4-one,

8-Methoxy-1- (3-methylbutyl) -5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one, 1-propyl-8-one methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one,

1-Isobutyl-8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-chi

2-one,

8-Methoxy-1-phenethyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one, and

1- (4-phenylthiomethyl) benzyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one.

The carbostyril compound of Formula (1) according to the present invention includes stereoisomers, optical isomers, hydrates and similar solvents thereof.

Among the compounds of the present invention, those having a basic group or groups can easily form salts with common pharmaceutically acceptable acids. Examples of such acids include hydrochloric acid, hydrobromic acid, nitric acid, sulfuric acid, phosphoric acid and other inorganic acid, methanesulfonic acid, p-toluenesulfonic acids, acetic acid, citric acids, tartaric acid, maleic acid, fumaric acid, acid malic acid, lactic acid and other organic acid, etc.

Among the compounds of the present invention, those having an acidic group or groups can easily form salts by reacting with basic pharmaceutically acceptable compounds. Examples of such basic compounds include sodium hydroxide, potassium hydroxide, calcium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogen carbonate, potassium hydrogen carbonate, etc.

The following is an explanation of pharmaceutical preparations comprising the compound of the present invention as an active ingredient.

Such pharmaceutical preparations are obtained by formulating the compound of the present invention into the usual pharmaceutical preparations using generally employed excipients or diluents such as fillers, extenders, binders, wetting agents, disintegrants, lubricants, etc. The form of such pharmaceutical preparations may be selected in various ways according to the purpose of therapy. Typical examples include tablets, pills, powders, solutions, suspensions, emulsions, granules, capsules, suppositories, injections (solutions, suspensions, etc.) and the like.

To form tablets, any of the various vehicles used

may be used, including, for example, lactose, white sugar, sodium chloride, glucose, urea, starch, calcium carbonate, kaolin, crystalline cellulose and other excipients; water, ethanol, propanol, single syrup, glucose solutions, starch solutions, gelatin solutions, carboxymethylcellulose, shellac, methylcellulose, potassium phosphate, polyvinylpyrrolidone and other binders; dry starch, sodium alginate, agar powder, yaminaran powder, sodium hydrogencarbonate, calcium carbonate, polyoxyethylene sorbitan fatty acid esters, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose and others disintegrants; sugar, stearin, cocoa butter, hydrogenated oils and other disintegration inhibitors; quartenary ammonium base, sodium lauryl sulfate and other absorption promoters; glycerin, starch and other wetting agents; starch, lactose, kaolin, bentonite, colloidal silicic acid and other absorbents; purified talc, stearates, boric acid powder, polyethylene glycol and other lubricants; etc.

Such tablets may be coated with usual coating materials as required to prepare, for example, sugar-coated tablets, gelatin-coated tablets, enteric-coated tablets, film-coated tablets, multilayer or double-layer tablets, etc.

To form pills, any of several known carriers may be used, including, for example, glucose, lactose, starch, cocoa butter, hydrogenated vegetable oils, kaolin, talc and other excipients; gum arabic powder, tragacanth powder, gelatin, ethanol and other binders; laminaran, agar and other disintegrants; etc.

To form suppositories, any of several known carriers may be used, including, for example, polyethylene glycol, cocoa butter, higher alcohols, esters of higher alcohols, gelatin, semi-synthetic glycerides, etc.

To form an injection, a solution, emulsion or suspension is sterilized and preferably isotonic with blood. Any of the various widely known diluents used may be employed to prepare the solution, emulsion or suspension. Examples of such diluents include water, ethanol, propylene glycol, ethoxylated isostearyl alcohol, polyoxylated isostearyl alcohol, polyoxyethylene sorbitan fatty acid esters, etc. In this case, the pharmaceutical preparation may contain sodium chloride, glucose or glycerin in an amount sufficient to prepare an isotonic solution, and may contain usual analgesic agents, buffers, solubilizers, etc., and others, if necessary, coloring agents. , flavorings, preservatives, sweetening agents, etc., and / or other medicines.

The proportion of the compound of the present invention in the pharmaceutical preparation is not limited and may be suitably selected from a wide range. It is generally preferred that the pharmaceutical preparation contains the compound of the present invention in a ratio of 1 to 70% by weight.

The routine of administration of the pharmaceutical preparation according to the present invention is not limited, and the preparation is administered by a routine suitable for the preparation form, patient gender and age, disease conditions, and other conditions. For example, tablets, pills, solutions, emulsions, granules and capsules are orally administered. Injections are intravenously administered alone or mixed with injection transfusions such as glucose solutions, amino acid solutions or the like, or administered alone intramuscularly, intracutaneously, subcutaneously or intraperitoneally as required. Suppositories are intraretally administered.

The dosage of the pharmaceutical preparation is suitably selected according to the patient's method of use, gender and age, severity of the disease, and other conditions, and is generally about 0.001 to about 100 mg / kg. kg body weight / day, and preferably 0.001 to 50 mg / kg body weight / day, in single or divided doses.

Since various dosages depending on various conditions, a dosage lower than the above range may be sufficient or a dosage greater than the above range may be required.

The present invention therefore provides a pharmaceutical composition.

comprising the carbostyril compound as an active ingredient for the therapy and prophylaxis of various diseases associated with NF-κΒ and a method for therapy and prophylaxis.

Diseases to be treated or prevented by the therapeutic / prophylactic composition of the invention are diseases associated with NF-κΒ, that is, diseases caused by unwanted activation of genes under NF-κΒ transcriptional regulatory factor control. Examples of such diseases include ischemic diseases, inflammatory diseases, autoimmune diseases, cancer invasion and metastasis, and cachexia. Examples of ischemic diseases include ischemic organ diseases (eg, ischemic heart diseases such as myocardial infarction, acute heart failure, chronic heart failure, etc., ischemic brain diseases such as cerebral infarction, ischemic lung diseases such as pulmonary infarction), symptom exacerbation after organ transplantation or organ surgery (for example, symptom exacerbation after heart transplantation, heart surgery, kidney transplantation, kidney surgery, liver transplantation, liver surgery, bone marrow transplantation, skin graft, corneal transplantation, and lung transplantation), reperfusion disorders, and post PTCA restenosis. Examples of inflammatory diseases include various inflammatory diseases such as nephritis, hepatitis, arthritis, etc., acute renal failure, chronic renal failure, and arteriosclerosis. Examples of autoimmune diseases include, but are not limited to, rash, multiple sclerosis, and Hashimoto's thyroiditis.

The pharmaceutical composition containing the carbostyril compound according to the present invention as an active ingredient is particularly suited for the therapy and prophylaxis of reperfusion disorders in ischemic diseases, exacerbation of symptoms after organ transplantation or organ surgery, post restenosis. -PTCA, cancer invasion and metastasis, and cachexia such as weight loss followed by the onset of cancer.

Carbostyryl compounds (1) of the present invention or salts thereof have COX-2 inhibitory activity and are thus useful as COX-2 inhibitors. More specifically, the carbostyril compound (1) or salts thereof have COX-2 production inhibitory activity and are therefore useful as COX-2 production inhibitors.

Due to the COX-2 inhibitory activity, the carbostyril compound (1) or salts thereof exhibit radiosensitivity enhancing effects on radiotherapy for cancer patients, and inhibitors of tumor activity-induced angiogenesis. Therefore, the carbostyril compound (1) or salts thereof are useful as radiotherapy radiosensitivity enhancers, or as inhibitors of tumor-induced angiogenesis. In addition, due to activity, carbostyril compound (1) or salts thereof are useful as anticancer effect boosters in radiotherapy or chemotherapy. As used herein, the term "chemotherapy" refers to a method of treating or preventing a tumor using an antitumor agent. Examples of anti-tumor agents include those which may be used in the medical field, such as cisplatin, paclitaxel, anastrozole, calcium carbonate, capecitabine, carboplatin, CP-461 cell reaction series, docetaxel, doxorubicin, etoposide. aids, fluoxymesterone, gemcitabine, goserelin, irinotecan, ketoconazole, ethozole, leucovorin, Levaisol, megestrol, mitoxantrone, raloxifene, reticuric acid, tomoxifen, thiotepa, topotecan, toremifene, vinorelin selenin, vinenethine, vinenethine, selenin ), sulindac sulfone, exemestane, eflornithine (DFMO), etc.

Examples of cancers to be treated or prevented include advanced malignancy, amyloidosis, neuroblastoma, meningioma, hemangiopericytoma, multiple brain metastasis, glioblastoma multiforme, glioblastoma, brain stem glioma, poor prognostic malignant tumor, amlign glioma, anaplastic astrocytoma. , anaplastic oligodendroglioma, neuroendocrine tumors, rectal adenocarcinoma, colorectal cancer Dukes C & D, nonresectable colorectal carcinoma, mystatic hepatocellular carcinoma, Kaposi's sarcoma, acute myeloblastic leukemia of karyotype, non-Hodgkin's Iodine , Cutaneous T-cell lymphoma, Cutaneous B-cell lymphoma, Diffuse large B-cell lymphoma, Low-grade follicular lymphoma, Malignant melanoma, Malignant mesothelioma, Malignant pleural effusion mesothelioma syndrome, Peritoneal carcinoma, Serous carcinoma papi - home, gynecological sarcoma, soft tissue sarcoma, scleroderma, cutaneous vasculitis, histiocytosis of Langerhans cell, leiomyosarcoma, progressive ossifying fibrodysplasia, hormone refractory prostate cancer, resected high-risk soft tissue sarcoma, non-resectable hepatocellular carcinoma, Waldenstrom macroglobulinaemia, smoldering myeloma, indolent myeloma, prostate cancer, independent, androgen-dependent stage IV non-metastatic prostate cancer, hormone-intensive prostate cancer, chemotherapy-intensive prostate cancer, papillary thyroid carcinoma, thyroid follicular carcinoma, medullary thyroid carcinoma, and leiomyoma.

Due to the inhibitory activity of COX-2, carbostyrin (1) compound or salts thereof are useful as therapeutic or preventive agents for COX-2-associated disorders and diseases, such as pain (chronic or acute pain), fever, inflammation, etc. COX-2- associated disorders and diseases are well known in the art to which the present invention belongs. Examples of COX-2-associated disorders and diseases include rheumatic fever; diseases associated with influenza or other virus infections, such as a cold; low back and cervical pain; Headache; toothache; bad form and injury; myositis; sympathetically independent pain; synovitis; arthritis, including rheumatoid arthritis; degenerative joint diseases, including osteoarthritis; gout and hookworm spondylitis; tendonitis; skin conditions such as psoriasis, eczema, sunburn and dermatitis; injuries such as sports injuries; and disorders originated from dental treatment or surgery.

Carbostyril Compound (1) or salts thereof are also useful as therapeutic or preventative agents for neurogenic pain. The neuropathic pain syndrome occurs after nerve injury. Even after the original injury has healed, the resulting pain may continue for several months or years. Neuropathic pain may occur in a certain region of a peripheral nerve, a dorsal root, the spinal cord, or the brain. Neuropathic pain syndromes are originally classified according to the disease or disorder causing the syndrome. Examples of neuropathic pain syndromes include diabetic neuropathy; nonspecific low back pain; multiple sclerosis pain; fibromyalgia; HIV-associated neuropathy; neuralgia such as post herpes neuralgia, or trigeminal nerve neuralgia; and pain caused by physical trauma, incision, cancer, poison, or acute inflammation.

Therefore, the carbostyril compound (1) or salts thereof are useful as anti-inflammatory agents, analgesics, etc., and may be administered separately or together with other COX-2 inhibitors, such as anti-inflammatory, analgesic agents, etc. . Best Mode for Carrying Out the Invention

The following examples illustrate the invention in greater detail.

them.

Example 1

Effects of test compounds on COX-2 gene expression in MKN-45 gastric cancer cell line

MKN-45 human gastric cancer cell line obtained from JCRB (Japanese Research Bioresources collection) was grown in Iscove's Modified Dulbecco's Medium (GIBCO product) containing 10% fetal calf serum for 24 hours using a 6-well plate. wells and a 5% CO2 incubator (37 ° C, 5% CO2). Test compound solutions by diluting each test compound with DMSO (solvent) to a final concentration of 1 μΜ, and the same amount of DMSO as a control solution (containing no test compound) were added to the wells. 6-well plates, and the cells were cultured in a CO2 incubator (37 ° C, 5% CO2) for 16 hours.

Cells were recovered, and RNATotaI was prepared. RNA was prepared from cells using Trizol reagent (Invitrogen product) according to the standard method. Real-time PCR was performed using TaqManO Gene Expansion Assays for human COX-2 (Applied Biosystems product), and the amount of COX-2 mRNA in each cell treated by test compound was determined.

The amount of COX-2 mRNA in cells treated by test compound was expressed as a percentage relative to that in control cells fixed as 100% to determine the percentage inhibition of COX-2 gene expression by each test compound. Each experiment was performed in triplicate, and the average of the three results was recorded.

The test compounds used in the experiments are as follows:

THE

^ 261

(La)

Test compound A: compounds of Formula (1a) wherein R 1 is methyl Test compound B: compounds of Formula (1a) wherein R 1 is isopentyl Test compound C: compounds of Formula (1a) wherein R 1 is 2-phenylethyl (in all above test compounds, R2ei is methyl and R651 is hydrogen).

Test compounds AaC were prepared in the same manner as in Examples 960, 965, and 978 of WO2006 / 035954, respectively.

Table 1 shows the results:

Table 1

Test compound COX-2 gene expression inhibition (%) Test compound A> 20 Test compound B> 20 Test compound C> 20

Real time PCR was performed under the following conditions. Real Time PCR Conditions

a) Preparation of standard solutions for COX-2 mRNA and beta-actin mRNA calibration curves

Standard COX-2 mRNA and beta-actin mRNA solutions were prepared according to the ABI PRISM 7000 Sequence Detection System User's Guide (Chapter 6 Analysis Assay). More specifically, the amounts of COX-2 mRNA and beta-actin mRNA in all cell samples were preliminarily determined, and samples containing the highest levels of COX-2 mRNA and beta-actin mRNA. between solvent control cell samples (samples with the smallest boundary cycle (Ct) value as determined based on fluorescence detection using the ABI PRISM 7000 Sequence Detection System (Applied Biosystems product)) were selected and used. as standard solutions, respectively. Subsequently, dilution series of each standard dissolution were prepared to form a calibration curve of COX-2 mRNA and beta-actin mRNA levels. When inclusion of all test samples in the calibration curve was found to be possible, a sample with the smallest boundary cycle (Ct) value among the cell treated by test sample was used as a standard solution to prepare a series of dilution. In dilution of standard solutions, DEPC treated water was used.

b) PCR reaction

PCR was performed according to manufacturers' instructions for the TaqMan® Gene Expression Assays (Applied Biosystems product). More specifically, 12.5 L of TaqMan® Universal PCR Master Mix, 1.25 Dl of Gene TaqMan® Expression Assays for COX-2 mRNA, and 11.25 Dl of cDNA solution, which was obtained. in a manner similar to that of 3) of Example 3 described below, were added to each sample in a 96-well plate ("MicroAmp® 96-well Optical Reaction Plate", product of Applied Biosystems), and shaken. A PCR reaction consisting of 50 ° C for 2 minutes and 95 ° C for 10 minutes, followed by 40 cycles consisting of 95 ° C for 15 seconds and 60 ° C for 1 minute was performed using a real time PCR device ( "ABI PRISM 7000 Sequence Detection System", product of Applied Biosystems) with data analysis software ("ABI PRISM 7000 SDS v1.1", product of Applied Biosystems). The amount of each mRNA was determined from the calibration curve using the ABI PRISM 7000 Sequence Detection System.

c) Correction of COX-2 mRNA amount

The amount of COX-2 mRNA was expressed relative to the amount of beta-actin mRNA using Excel 2000 (product of Microsoft Corporation), and used for data analysis. Example 2

NF-kappaB Reporter Test

(1) Preparation of pNF-kappaB-SEAP

pNF-kappaB-SEAP was obtained from Clonetech Laboratories Inc.

(2) MKN-45 Cell Cultivation

Ciropreserved MKN-45 cells (JCRB (Japanese Collection of Research Bioresources) product) were thawed and cultured in a standard medium in an incubator (37 ° C, 5% CO 2). Every three to five days, the cells were recovered by treatment with Tripsin-EDTA, then properly diluted and subcultured. Two or more subcultured MKN-45 cells with a survival rate of 95% or more were used in each experiment.

(3) Cell seeding

Subcultured MKR-45 cells were harvested using solu-

Tripsin-EDTA, and several viable cells were counted. Cells were suspended in a standard medium to produce a suspension of 1.5 x 105 cells / mL. A 24-well plate was seeded with 500 μL / well of the cell suspension, and the cells were cultured in an incubator (37 ° C, 5% CO2).

(4) Transfection

On the day after sowing, transfection was performed according to the following protocol.

(4.1) Preparation of 4 μΙ_ 0.1 μg / μL plasmid solution of pNFkappaB-SEAP were placed in

each well and diluted with 50 μΙ_ of OPTI-MEM I (Invitrogen Japan K.K. product) by mixing by inversion. (4.2) Preparation of Lipofectamine Dilution

1 μι. Lipofectamine 2000 reagent (Invitrogen product) was placed in each well and diluted with 50 μΐ of OPTI-MEM I (product from Life Technologies Inc.) mixing by inversion. The mixture was allowed to stand at room temperature for 5 to 10 minutes to prepare a lipofectamine dilution.

(4.3) Preparation of transfection mixture

Plasmid solution and Lipofectamine dilution were mixed by inversion and allowed to stand at room temperature for 20 to 30 minutes to prepare a transfection mixture.

(4.4) Addition to cells

Culture medium was removed from the 24-well plate by suction. While care was taken not to dry MKN-45 cells, the inner surface of the wells was washed with 1 ml well of PBS. After the medium was replaced with 500 µL well of OPTI-MEM I (product from Life Technologies Inc.), 100 µL well of the transfection mixture was added, and cells were cultured in an incubator (37 ° C, 5% CO2). After about 5 hours of incubation, the medium was replaced with a standard medium, and the cells were also cultured in a CO2 incubator (37 ° C, 5% CO2) until the following day.

(5) Addition of test or control compound

The next morning, the culture medium supernatant was removed by suction and replaced with 1 mCavity of the test compound solution or control solution diluted with a standard medium. The cells were cultured in a CO2 incubator (37 ° C, 5% CO2) for 1 hour. Each experiment was performed in triplicate.

(6) Addition of Stimulus

200 ng / mL IL-Iβ was added in an amount of μLycavity (final concentration: 2 ng / mL), and cells were cultured in a CO2 incubator (37 ° C, 5% CO2) for 6 hours.

(7) Reporter test

A Reporter Assay was performed using Assay Kit-SEAP Reporter (Toyobo Co. product) according to Manufacturer's protocols.

More specifically, 500 µl of the culture broth was transferred into a tube and centrifuged at 15,000 rpm for 5 minutes at 4 ° C. The supernatant was transferred to a 96-well white plate. The positive control included with the Assay Kit-SEAP Reporter, and a standard medium such as a blank control were added in an amount of 20 μL / well to the 96-well white plate. Also, an inhibitor to inhibit the AP activity of MKN-45 cells was added in an amount of 20 μL'cavity. After sealing the plate, the contents were mixed with the cavity. The plate was placed in a CO2 incubator (37 ° C, 5% CO2) and allowed to stand for 30 minutes. Subsequently, the plate was allowed to stand on ice for 1 minute, followed by the addition of 160 μL / well of Lumi-Phos Plus (a chemiluminescent substrate, product from Lumigen Inc.). The plate was resealed and placed in a light protected state in a CO2 incubator (37 ° C, 5% CO2). After the plate was allowed to stand for 15 to 30 minutes, luminescence was assessed for about 5 to about 10 seconds using a luminometer.

(8) Results

The results of the reporter test were expressed as Control Percentage (or inhibition), calculated according to the following formulas. The luminescence of each sample was calculated by subtracting the average of White samples.

Results indicate that the carbostyril compound (I) or a salt thereof has an inhibitory activity against NF-kB activity.

(Luminescence of cells treated by test compound, stimulated by IL-Ιβ-)

(PercentageControIe) = - χ 100

(Luminescence of 1L-1 β-stimulated DMSO-treated cells) Test compound Ί IL-1b (+) SE DMSO medium (0.05%) (control) 1.00 0.084 025 0. H ■ VN A> = 0 k ^ -CO2Me 0.58 0.037 123 VB SS lXX 0.46 0.035 125 X> = o ~ XX CN 0.55 0.044 127 YU ~ "α» 0.60 0.066 131 χ-SS lCl 0.49 0.047 134 0 H • VN kO 0.46 0.040 233 VW H 0.85 0.054 234 0. H f- ^ S Tl S 0.67 0.044 H "D 237 V" X ^ 0 Vi 0.57 0.009 608 Uo Me- O L 0.71 0.062 Vo 612 Uo "" Vcri F 0.67 0.054 613 Uo I ^ -S Me-O L 0.86 0.050 V-O 616 ηΠ. 0.57 0.029 914 X> = s' 1C ^ 0 .53 0.029 965 YU Me-O 0.68 0.027 971 VH T> = S kCO 0.56 0.005 980 ° v. VN X> = s kXX 0.59 0.023 995 0.66 0.056 996 0.43 0.020

* 1: Example No, from W02006 / 035954

Example 3

1) RNA extraction

RNA was extracted from the cells used in Example 2 according to the manufacturing protocol for ABI Prism 6100 Nucleic Acid PrepSation (a nucleic acid isolation system, product of Applied Biosystems). More specifically, after removal of the supernatant and washing with 1 mL PBS, 250 DL Nucleic Acid Purification Lysis Solution (Part No. 4305895, Applied Biosystems) were added, and then stirred using a shaker for 2 to 5 minutes. 3 minutes. The lysate solution containing the cell lysate was collected, and the total amount was transferred to the wells of the RNA Purification Tray (Part No. 4305673, Applied Biosystems), which was pre-moistened with 40 DL Purification Wash Solution. Nucleic Acid I (Part Nos. 4305891, Applied Biosystems) in advance. Aspiration (20% pressure) was performed for 2 minutes to absorb the sample onto the RNA Purification Tray, followed sequentially by addition and aspiration (20% pressure, 2 minutes) of 500 µL Wash Solution I , Nucleic Acid Purification (Part No. 4305891, Applied Biosystems), 400 µl Washing Solution II, Nucleic Acid Purification (Part No. 4305890, Applied Biosystems Product), 400 μι. Wash Solution II, and 300 μι. of the Il Wash Solution in that order. Aspiration (90% pressure) was performed for 5 minutes to remove the water content from the RNA Purification Trays. After addition of 150 μΙ_ of Elution Solution, Nucleic Acid Purification (Part No. 5305893, Applied Biosystems product), aspiration (20% pressure) was performed for 2 minutes during flow collection. This was used as a collected RNA solution.

2) Determination of RNA concentration

The absorbance of the RNA solution collected at 260 nm was evaluated

using a microplate spectrophotometer ("SpectraMax Plus", Molecular Devices product) with analysis software ("SOFTmaxPRO ver.3.1.2", product of Molecular Devices), and the RNA concentration was determined from the absorbency. Also, absorbance at 280 nm was assessed and RNA purity was determined using the analysis software.

3) cDNA Preparation

cDNA was synthesized according to the manufacturing protocol for TaqMan® Reverse Transcription Reagents (Part Ns No. 808-0234, Applied Biosystems product). More specifically, about 0.5 μρ RNA, 2.5 μΙ_ from 10 χ RT buffer, 5.5 μΙ_ MgCl2 solution, 5 μι. dNTP mix, 1.25 μΙ_ of random hexamer (primers), 0.5 μΐ_ of RNase1 inhibitor and 0.63 μΙ_ of MuItiScribe Reverse Transcriptase (Applied Biosystems product) were added to each sample RNA collected. in a tube, and DEPC-treated water was added to make a total volume of 25 μΙ_ and stirred. A reaction consisting of 25DC for 10 minutes, 48DC for 30 minutes, and 95DC for 5 minutes was performed using a PCR thermal cycle ("TaKaRa PCR Thermal Cycle Dice", Takara Bio Inc. product) for prepare a cDNA solution.

4) Real time PCR PCR reaction

PCR was performed according to the manufacturing protocol for TaqMan® Gene Expression Assays (Applied Biosystems product). More specifically, 5 μΙ_ TaqMan® Fast Universal PCR Master Mix (Applied Biosystems product), 0.5 μΐ_ TaqMan® Gene Expression Assays for the target gene (gene specific probe and primer series, product Applied Biosystems), and 4.5 μΙ_ of the cDNA solution obtained above were added to each sample and shaken. A PCR reaction consisting of heating at 95 ° C for 20 seconds, followed by 40 cycles consisting of heating at 95 ° C for 3 seconds and annealing and extension at 60 ° C for 30 seconds was performed using a Real Time PCR Device ("Applied Biosystems 7500 Real Time System PCR") with SDS Software v1.4 (Applied Biosystems Product). Input cycle values (Ct) were calculated using the software.

TaqMan® Gene Expression Assays Assay IDs for the target genes used are as follows: Hs00153133_m1 for COX2

Hs00174128_m1 for TNFa Hs00174103_m1 for IL-8 Hs99999902_m1 for ACTB

5) Method for determining mRNA Expression Levels

relative

The expression level of each gene was determined according to the following formula using the ACTB level as a reference standard.

(Relative mRNA expression level) = 2A - {(Target gene Ct value) - (ACTB Ct value)}

Relative mRNA expression levels obtained by various pharmacists were determined by fixing the relative mRNA expression level in IL-1-stimulated DMSO-treated MKN-45 cells as 100%.

Results indicate that the carbostyril compound (I) or a

its salt has a COX-2 inhibitory activity agonist, TNF-α, and / or IL-8, particularly a production of COX-2 inhibitory activity agonist, TNF-α, and / or IL-8, more particularly a COX-2, TNF-α, and / or IL-8 inhibitory activity agonist gene expression.

Meiso SD Ne. Compounds * 1 IL-1 COX2 TNFα IL-8 COX2 TNFα IL-8 DMSO (0.05%) + 100.0% 100.0% 100.0% 4.0% 11.5% 16.7% 025 + 38.3% 53.0% 59.9% 4.8% 10.9% 1.7% 123 + 28.6% 28.5% 48.3% 2.7% 7.6% 16.6% 125 + 29.2% 52.5% 45.4% 3.3% 2.3% 3.7% 127 + 31.0% 49.8% 44.8% 1.3% 10.5% 8, 0% 131 + 80.9% 71.3% 77.9% 3.0% 10.9% 9.7% 134 + 33.1% 36.6% 55.4% 5.9% 2.6% 2.4% 150 + 53.7% 53.9% 52.0% 2.8% 18.8% 0.9% 159 + 27.7% 33.5% 34.0% 3.6% 4, 5% 1.2% 164 + 21.7% 30.0% 24.8% 2.8% 9.1% 3.1% 186 + 29.7% 70.8% 67.7% 11.8% 18.0% 3.7% 225 + 32.9% 44.6% 50.0% 3.3% 10.7% 9.7% 232 + 29.9% 28.9% 33.8% 5, 7% 10.1% 5.7% 233 + 24.9% 28.9% 30.4% 1.8% 10.7% 0.8% 234 + 24.0% 32.4% 28.3% 2.2% 15.6% 1.8% 237 + 25.9% 26.2% 25.9% 5.4% 18.6% 4.9% 608 + 42.4% 30.8% 36, 5% 4.0% 7.6% 2.9% 612 + 33.4% 31.1% 41.8% 6.8% 6.9% 3.7% 613 + 112.4% 94.0% 91.5% 7.4% 17.9% 6.5% 616 + 26.3% 31.4% 35.3% 2.0% 8.3% 2.8% 914 + 32.9% 66, 7% 61.9% 5.1% 27.1% 5.1% 965 + 37.6% 63.0% 61.2% 4.3% 13.7% 1.5% 971 + 30.8% 63.4% 55.9% 6.5% 22.1% 4.5% 9 80 + 53.8% 98.0% 79.4% 8.2% 8.9% 6.3% 981 + 37.8% 75.7% 70.4% 5.0% 17.1% 9, 1% 993 + 27.6% 46.8% 45.6% 3.8% 21.5% 8.7% 995 + 28.1% 29.3% 38.3% 2.5% 7.2% 2.4% 996 + 31.3% 41.3% 50.1% 4.5% 11.4% 0.1%

* 1: Example W02006 / 035954

Claims (19)

1.  Preventive or therapeutic agent for a disease associated with NF-κΒ,  characterized in that it comprises as an active ingredient a carbostyril compound represented by General Formula (1) or a salt thereof,   where A is a direct link,  a lower alkylene group,  or a lower alkylidene group;   X is an oxygen atom or a sulfur atom;   the bond between positions 3 and 4 of the carbostyril backbone is a single bond or a double bond;   R4 and R5 each represents a hydrogen atom,  provided that when the bond between positions 3 and 4 of the carbostyril backbone is a double bond,  R4 and R5 may instead be linked together as a group -CH = CH-CH = CH-;   phenyl ring with one or more members selected from the group consisting of a phenyl group,  lower alkyl groups,  lower alkoxy groups,  halogen atoms,  groups - (B) 1NR6R7,  a nitro group,  a carboxy group,  lower alkoxycarbonyl groups,  a cyan group,  phenyl lower alkoxy groups,  a phenoxy group,  piperidinyl lower alkoxycarbonyl groups,  lower alkoxycarbonyl amino groups optionally substituted by one or more cycloalkyl groups,  2-imidazolinylcarbonyl groups optionally substituted on the 2-imidazoline ring with one or more lower alkylthio groups,  optionally substituted 3-pyrrolinylcarbonyl groups on the 3-pyrroline ring with one or more lower alkyl groups,  optionally substituted thiazolidinylcarbonyl groups on the thiazole ring (1) R 1 is one of the following (1 -1) to (1-30):  (1-1) a hydrogen atom,  (1-2) a lower alkyl group,   (1-3) a lower alkyl phenyl group optionally substituted on dyne with a phenyl group,  3-azabicyclic groups [3, 2, 2] nonylcarbonyl,  piperidinyl lower alkyl groups,  lower alkyl anilino groups optionally substituted on the amino group with one or more lower alkyl groups,  phenyl lower alkyl groups,  indolinyl lower alkyl groups,  and piperidinylcarbonyl groups optionally substituted on the piperidine ring with one or more lower alkyl groups,   (1-4) a lower cycloalkyl alkyl group,   (1-5) a lower alkyl phenoxy group,   (1-6) a lower alkyl naphthyl group,   (1-7) a lower alkyl lower alkoxy group,   (1-8) a lower alkyl carboxy group,   (1-9) a lower alkyl alkoxycarbonyl group,   (1-10) a lower alkyl pyridyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of halogen atoms;  piperidinyl groups;  a morpholino group;  piperazinyl groups optionally substituted on the piperazine ring with one or more members selected from the group consisting of a phenyl group and lower alkyl group;  thienyl groups;  a phenyl group;  pyridyl groups;  piperidinyl lower alkyl groups;  phenyl lower alkyl groups;  biphenyl groups;  lower alkyl groups optionally substituted with one or more halogen atoms;  pyridylamino groups;  pyridylcarbonylamino groups;  lower alkoxy groups;  lower alkyl anilino groups optionally substituted on the amino group with one or more lower alkyl groups;  and anilino groups optionally substituted on the amino group with one or more lower alkyl groups,   (1-14) a phenyl group,   (1-15) a lower alkyl quinolyl group,   (1-16) a lower alkyl group substituted by lower alkoxy al- (1-11) a lower alkyl cyano group,  (1-12) a group -ArCONR8R9,  (1-13) a group of the following loweroxy formula,   (1-17) a lower alkyl group substituted by hydroxy,  (1-18) a thiazolyl lower alkyl group optionally substituted on the triazole ring with one or more members selected from the group consisting of halogen atoms,  a phenyl group,  tienila groups,  and pyridyl groups,   (1-19) a lower alkyl group optionally substituted with one or more halogen atoms,   (1-20) a lower alkyl alkylsioxy group,  (1-21) a lower alkyl phenoxy group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms;  lower alkoxy groups;  halogen atoms;  lower alkenyl groups;  cycloalkyl groups;  a nitro group;  and a phenyl group,   (1-22) a lower alkyl phenylthio group optionally substituted on the phenyl ring having one or more halogen atoms,   (1-23) piperidinyl lower alkyl groups optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl phenyl groups and one phenyl group,   (1-24) a lower alkyl piperazinyl group optionally substituted on the piperazine ring with one or more phenyl groups,   (1-25) a group 1, 2, 3, 4-tetrahydroisoquinolyl lower alkyl,  (1-26) a lower alkyl naphthyloxy group,   (1-27) a lower alkyl benzothiazolyloxy group optionally substituted on the benzothiazole ring with one or more alkyl groups,   (1-28) a lower alkyl group substituted with one or more members selected from the group consisting of quinolyloxy groups and isoquinolyloxy groups,   (1-29) a lower alkyl pyridyloxy group optionally substituted on the pyridine ring with one or more lower alkyl groups,   (1-30) a lower alkenyl;   R2 is one of the following (2-1) to (2-33):  (2-1) a hydrogen atom,     (2-2) a lower alkoxy group,  (2-3) a lower alkyl group,  (2-4) a lower alkoxy carboxy group,  (2-5) a lower alkoxy lower alkoxycarbonyl group,   (2-6) a hydroxy group,   (2-7) a phenyl lower alkoxy group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms;  lower alkyl groups optionally substituted with one or more halogen atoms;  lower alkylthio groups optionally substituted with one or more halogen atoms;  lower alkoxy groups;  a nitro group;  lower alkylsulfonyl groups;  lower alkoxycarbonyl groups;  phenyl lower alkenyl groups;  lower alkanoyloxy groups;  and groups 1, 2, 3-thiadiazolyl,   (2-8) a piperidinyl lower alkoxy group optionally substituted on the piperidine ring with one or more lower alkyl groups,   (2-9) an amino-substituted lower alkoxy group optionally substituted by one or more lower alkyl groups,  (2-10) a lower alkenyloxy group,   (2-11) a lower alkoxy pyridyl group optionally substituted on the pyridine ring with one or more lower alkyl groups,  each lower alkyl substituent optionally being substituted with one or more halogen atoms,   (2-12) a lower alkynyloxy group,  (2-13) a lower phenyl alkynyloxy group,   (2-14) a phenyl lower alkenyloxy group,   (2-15) a lower alkoxy furyl group optionally substituted on the furan ring with one or more lower alkoxycarbonyl groups,   (2-16) a tetrazolyl lower alkoxy group optionally substituted on the tetrazol ring with a member selected from the group consisting of a phenyl group,  lower alkyl phenyl groups,  and lower cycloalkyl alkyl groups,   (2-17) a group 1, 2, 4-oxadiazolyl lower alkoxy optionally substituted on ring 1, 2, 4-oxadiazole with a phenyl group,  the phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups,   (2-18) an isoxazolyl lower alkoxy group optionally substituted on the isoxazole ring with one or more lower alkyl groups,   (2-19) a lower alkoxy group 1, 3, 4-oxadiazolyl optionally substituted on ring 1, 3, 4-oxadiazole with a phenyl group,  the phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups,   (2-20) a lower alkoxy lower alkanoyl group,   (2-21) a thiazolyl lower alkoxy group optionally substituted on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and a phenyl group,  each phenyl substituent optionally being substituted on the phenyl ring with one or more halogen atoms,   (2-22) a piperidinoxy group optionally substituted on the piperidine ring with one or more benzoyl groups,  each benzoyl substituent optionally being substituted on the phenyl ring with one or more halogen atoms,    (2-23) a thienyl lower alkoxy group,   (2-24) a lower alkoxy phenylthio group,   (2-25) a carbamoyl substituted lower alkoxy group optionally substituted with one or more lower alkyl groups,  (2-26) a lower alkoxy benzoyl group,   (2-27) a lower alkoxy pyridylcarbonyl group,   (2-28) an imidazolyl lower alkoxy group optionally substituted on the imidazole ring with one or more phenyl lower alkyl groups,  (2-29) a lower alkoxy phenoxy group,   (2-30) a lower alkoxy group substituted by phenyl lower alkoxy,   (2-31) a group 2, 3-dihydro-1H-indenyloxy,   (2-32) an isoindolinyl lower alkoxy group optionally substituted on the isoindoline ring with one or more oxo groups,     (2-33) a phenyl group;  R3 is one of the following (3-1) to (3-19):  (3-1) a hydrogen atom,  (3-2) a lower alkyl group,  (3-3) a hydroxy-substituted lower alkyl group,  (3-4) a lower cycloalkyl alkyl group,  (3-5) a lower alkyl carboxy group,  (3-6) a lower alkyl alkoxycarbonyl group,  (3-7) a phenyl lower alkyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms;  lower alkyl groups optionally substituted with one or more halogen atoms;  lower alkoxy groups optionally substituted with one or more halogen atoms;  a phenyl group;  lower alkoxycarbonyl groups;  a phenoxy group;  lower alkylthio groups;  lower alkylsulfonyl groups;  phenyl lower alkoxy groups;  and nitro groups optionally substituted by one or more lower alkanoyl groups,  (3-8) a lower alkyl naphthyl group,   (3-9) a lower alkyl furyl group optionally substituted on the furan ring with one or more lower alkoxycarbonyl groups,   (3-10) a thiazolyl lower alkyl group optionally substituted on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and a phenyl group,  each phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups optionally substituted by halogen,   (3-11) a lower alkyl tetrazolyl group optionally substituted on the tetrazol ring with one or more lower alkyl groups,  (3-12) a lower alkyl benzothienyl group optionally substituted on the benzothiophene ring with one or more halogen atoms,  (3-13) a lower alkynyl group,  (3-14) a lower alkenyl group,  (3-15) a lower alkenyl phenyl group,  (3-16) a lower alkyl benzoimidazolyl group,     (3-17) a lower alkyl pyridyl group,   (3-18) a lower alkyl imidazole group optionally substituted on the imidazole ring with one or more phenyl lower alkyl groups,  (3-19) a quinolyl lower alkyl group;    B is a carbonyl group or an -NHCO- group;   I is 0 or 1;   R 6 and R 7 each independently represent one of the following (4-1) to (4-79):   (4-1) a hydrogen atom,   (4-2) a lower alkyl group,   (4-3) a lower alkanoyl group,   (4-4) a lower alkylsulfonyl group optionally substituted by one or more halogen atoms,   (4-5) an alkoxycarbonyl group optionally substituted by one or more halogen atoms,   (4-6) a lower alkyl group substituted by hydroxy,  (4-7) a pyridylcarbonyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of pyrrolyl groups and halogen atoms,   (4-8) a pyridyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of lower alkyl groups and lower alkoxy groups,   (4-9) a lower alkyl pyridyl group,   (4-10) a phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms;  lower alkyl groups optionally substituted with one or more halogen atoms;  a phenoxy group;  lower alkoxy groups optionally substituted with one or more halogen atoms;  lower alkylthio groups;  lower alkylsulfonyl groups;  amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups;  pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups;  piperidinyl groups optionally substituted on the piperidine ring with one or more lower alkyl groups;  lower alkenyl groups;  an aminosulfonyl group;  a hydroxy group;  carbamoyl groups optionally substituted by one or more lower alkyl groups;  phenyl lower alkoxy groups;  and a cyan group,   (4-11) a cycloalkyl group optionally substituted on the cycloalkyl ring with one or more lower alkyl groups,   (4-12) a benzoyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms;  a phenoxy group;  a phenyl group;  lower alkyl groups optionally substituted with one or more halogen atoms;  lower alkoxy groups;  lower alkanoyl groups;  a nitro group;  a cyan group;  amino groups optionally substituted with one or more members selected from the group consisting of a phenyl group and lower alkyl groups;  pyrrolidinyl groups optionally substituted on the pyrrolidine ring with one or more oxo groups;  pyrrolyl groups;  pyrazolyl groups;  groups 1, 2, 4-triazolyl;  and imidazolyl groups,   (4-13) a phenyl ring substituted benzoyl group with one or more lower alkylenedioxy groups,   (4-14) a cycloalkylcarbonyl group,   (4-15) a furylcarbonyl group,   (4-16) a naphthylcarbonyl group,   (4-17) a phenoxycarbonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxy groups,  lower alkyl groups,  halogen atoms,  and a nitro group,   (4-18) a lower phenyl alkoxycarbonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and a nitro group,   (4-19) a piperidinyl group optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl group;  lower alkanoyl groups;  optionally substituted benzoyl groups on the phenyl ring having one or more halogen atoms;  and optionally substituted phenyl groups on the phenyl ring having one or more halogen atoms,   (4-20) a lower alkyl tetrahydropyranyl group,  (4-21) a lower cycloalkyl alkyl group,   (4-22) a lower alkenyl group,   (4-23) a lower alkyl phenyl group optionally substituted on the alkyl group with one or more lower alkoxycarbonyl groups;  and optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms,  lower alkyl groups optionally substituted by one or more halogen atoms,  lower alkoxy groups optionally substituted by one or more halogen atoms,  and a hydroxy group,   (4-24) a lower alkylphenyl group substituted by lower alkylenedioxy,    (4-25) a lower alkyl furyl group,   (4-26) a lower alkyl carbamoyl group optionally substituted with one or more members selected from lower alkyl groups and a phenyl group,  each phenyl substituent optionally being substituted on the phenyl ring with one or more lower alkyl groups,   (4-27) a lower alkyl lower alkoxy group,   (4-28) a lower alkyl imidazole group optionally substituted on the lower alkyl group with one or more members selected from the group consisting of a carbamoyl group and lower alkoxycarbonyl groups,   (4-29) an amino-substituted lower alkyl group optionally substituted with one or more lower alkyl groups,   (4-30) a group 2, 3, 4, 5-tetrahydrofuryl optionally substituted on ring 2, 3, 4, 5-tetrahydrofuran with one or more oxo groups,  (4-31) a lower alkyl alkoxycarbonyl group,  (4-32) a lower alkyl pyrrolidinyl group optionally substituted on the pyrrolidine ring with one or more lower alkyl groups,  (4-33) a lower alkanoyl phenoxy group,  (4-34) a lower alkyl morpholino group,     (4-35) an indolyl group,  (4-36) a thiazolyl group,  (4-37) a group 1, 2, 4-triazolyl,  (4-38) a lower pyridyl alkanoyl group,  (4-39) a thienylcarbonyl group,  (4-40) a lower thienyl alkanoyl group,  (4-41) a lower cycloalkyl alkanoyl group,  (4-42) an isoxazolylcarbonyl group optionally substituted on the isoxazole ring with one or more lower alkyl groups,  (4-43) a pyrazylcarbonyl group,   (4-44) a piperidinylcarbonyl group optionally substituted on the piperidine ring with one or more members selected from a benzoyl group and lower alkanoyl groups,   (4-45) a chromanylcarbonyl group,   (4-46) a lower isoindolinyl alkanoyl group optionally substituted on the isoindoline ring with one or more oxo groups,   (4-47) a thiazolidinyl lower alkanoyl group optionally substituted on the thiazolidine ring with one or more members selected from an oxo group and a thioxo group,   (4-48) a piperidinyl lower alkanoyl group,  (4-49) a lower alkenylcarbonyl phenyl group optionally substituted on the phenyl ring with one or more halogen atoms,   (4-50) a phenyl phenyl lower alkenylcarbonyl group substituted with one or more alkylenedioxy groups,   (4-51) a pyridyl lower alkenyl carbonyl group,  (4-52) a lower alkanoyl pyridylthio group,  (4-53) an indolylcarbonyl group,  (4-54) a pyrrolylcarbonyl group,   (4-55) a pyrrolidinylcarbonyl group optionally substituted on the pyrrolidine ring with one or more oxo groups,  (4-56) a benzofurylcarbonyl group,  (4-57) an indolyl lower alkanoyl group,     (4-58) a benzothienylcarbonyl group,   (4-59) a phenyl lower alkanoyl group optionally substituted on the phenyl ring with one or more halogen atoms,   (4-60) a phenylsulphonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxycarbonyl groups;  a cyan group;  a nitro group;  optionally substituted nitro groups with one or more alkanoyl groups;  a hydroxy group;  a carboxyl group;  lower alkyl lower alkoxycarbonyl groups;  halogen atoms;  lower alkyl groups optionally substituted with one or more halogen atoms;  and lower alkoxy groups optionally substituted with one or more halogen atoms,   (4-61) a thiosulfonyl group optionally substituted on the thiophene ring with one or more members selected from the group consisting of halogen atoms and lower alkoxycarbonyl groups,   (4-62) a quinolylsulfonyl group,   (4-63) an imidazolyl sulfonyl group optionally substituted on the imidazole ring with one or more lower alkyl groups,   (4-64) a phenylsulfonyl group optionally substituted on the phenyl ring with one or more lower alkylenedioxy groups,   (4-65) a lower alkenylsulfonyl group,   (4-66) a lower cycloalkylalkylsulfonyl group,  (4-67) a group 3, 4-dihydro-2H-1, Optionally substituted 4-benzoxazinylsulfonyl on ring 3, 4-dihydro-2H-1, 4-benzoxazine with one or more lower alkyl groups,   (4-68) a pyrazolylsulfonyl group optionally substituted on the pyrazole ring with one or more members selected from halogen atoms and lower alkyl groups,   (4-69) an isoxazolyl sulfonyl group optionally substituted on the isoxazole ring with one or more lower alkyl groups,   (4-70) a thiazolylsulfonyl group optionally substituted on the triazole ring with one or more members selected from the group consisting of lower alkyl groups and one amino group,  each amino substituent optionally being substituted with one or more alkanoyl groups,  (4-71) a phenyl lower alkylsulfonyl group,  (4-72) a lower alkenylsulfonyl phenyl group,  (4-73) a naphthyloxycarbonyl group,  (4-74) a lower alkynyloxycarbonyl group,  (4-75) a lower alkenyloxycarbonyl group,  (4-76) a lower alkoxycarbonyl group substituted by phenyl lower alkoxy,   (4-77) a cycloalkyloxycarbonyl group optionally substituted on the cycloalkyl ring with one or more lower alkyl groups,  (4-78) a tetrazolyl group,   (4-79) an isoxazolyl group optionally substituted on the isoxazole ring with one or more lower alkyl groups;  or instead,   R6 and R7 may be linked together to form,  together with the nitrogen atom to which they are attached,  a group 1, 2, 3, 4-tetrahydroisoquinolyl,  an isoindolinyl group,  or a 5- to 7-membered saturated heterocyclic group,  the heterocyclic group optionally containing one or more additional heteroatoms and optionally being substituted with one to three members of the following (5-1) to (5-28):  (5-1) lower alkyl groups,  (5-2) lower alkoxy groups,  (5-3) an oxo group,  (5-4) a hydroxy group,  (5-5) lower alkyl pyridyl groups,   (5-6) phenyl groups optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms;  lower alkoxy groups optionally substituted with one or more halogen atoms;  lower alkyl groups optionally substituted with one or more halogen atoms;  a cyan group;  and a hydroxy group,  (5-7) lower alkylene phenyl groups substituted by lower alkylenedioxy,   (5-8) optionally substituted lower alkyl phenyl groups on the phenyl ring having one or more halogen atoms,  (5-9) pyrimidyl groups,  (5-10) pyrazyl groups,  (5-11) cycloalkyl groups,   (5-12) phenyl lower alkoxy groups optionally substituted on the phenyl ring having one or more halogen atoms,   (5-13) optionally substituted benzoyl groups on the phenyl ring having one or more halogen atoms,   (5-14) phenyl ring substituted benzoyl groups having one or more lower alkylenedioxy groups,   (5-15) lower alkylcarbamoyl groups optionally substituted by one or more members selected from the group consisting of a phenyl group and lower alkyl groups,   (5-16) benzoxazolyl groups,   (5-17) lower alkoxycarbonyl groups,   (5-18) a carbamoyl group,   (5-19) phenyl lower alkylidene groups optionally substituted on the phenyl ring having one or more halogen atoms,  (5-20) phenyl lower alkoxycarbonyl groups,   (5-21) optionally substituted pyridyl groups on the pyridine ring with one or more members selected from the group consisting of a cyano group and lower alkyl groups,   (5-22) lower alkyl furyl groups,  (5-23) tetrahydropyranyl groups,   (5-24) imidazolyl lower alkyl groups,   (5-25) naphthyl groups,  (5-26) groups 2, 3-dihydro-1H-indenyl,  (5-27) lower alkyl groups 1, 3-dioxolanil,  (5-28) groups - (A3) mNR11R12;   A 1 is a lower alkylene group;   R 8 and R 9 each independently represent one of the following (6-1) to (6-25):     (6-1) a hydrogen atom,  (6-2) a lower alkyl group,   (6-3) a phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms;  lower alkylthio groups;  lower alkoxy groups optionally substituted with one or more halogen atoms;  halogen atoms;  a phenyl group;  lower alkylammonium groups;  a cyan group;  a phenoxy group;  cycloalkyl groups;  pyrrolidinyl groups optionally substituted with one or more oxo groups;  groups 1, 2, 3, 4-tetrahydroisoquinolylcarbonyl;  groups 1, 2, 3, 4-tetrahydroquinolylcarbonyl optionally substituted with one or more lower alkyl groups;  groups 1, 2, 3, 4-tetrahydroquinoxalinylcarbonyl optionally substituted with one or more lower alkyl groups;  optionally substituted thiazolyl groups with one or more phenyl groups;  a carbamoyl group;   phenyl lower alkoxy groups;  lower alkylsulfonylamino groups;  anilino groups optionally substituted with one or more halogen atoms;  phenyl lower alkyl groups;  lower alkyl groups substituted by hydroxy,  (6-4) a cycloalkyl group,  (6-5) a lower cycloalkyl alkyl group,   (6-6) a lower alkyl carbamoyl group,   (6-7) a lower alkyl phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms;  lower alkoxy groups optionally substituted with one or more halogen atoms;  halogen atoms;  and a phenyl group,   (6-8) amino lower alkyl substituted by lower alkyl,  (6-9) a naphthyl group,  (6-10) a lower alkyl naphthyl group,  (6-11) a lower alkyl tetrahydronaphthyl group,   (6-12) a fluorenyl group,   (6-13) a pyridyl group,  (6-14) a lower alkyl pyridyl group,     (6-15) a pyrimidinyl group,   (6-16) a lower alkyl pyrazinyl group optionally substituted on the pyrazine ring with one or more lower alkyl groups,  (6-17) a thiazolyl group,   (6-18) a lower alkyl pyrazolyl group optionally substituted on the pyrazole ring with one or more lower alkyl groups,  (6-19) a lower alkyl thienyl group (6-20) a piperidinyl group optionally substituted on the piperidine ring with one or more members selected from the group consisting of lower alkyl group;  a benzoyl group;  and optionally substituted lower alkyl phenyl groups on the phenyl ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups,  (6-21) an indolyl group,  (6-22) an indazolyl group,   (6-23) a group 3, 4-dihydrocarbostyryl optionally substituted with one or more lower alkyl groups,   (6-24) a quinolyl group optionally substituted by one or more lower alkyl groups,   (6-25) a carbazolyl group optionally substituted with one or more lower alkyl groups;  or R8 and R9 may be linked together to form,  together with the nitrogen atom to which they are attached,  a 5- or 8-membered saturated heterocyclic group optionally containing one or more additional heteroatoms and optionally substituted on the heterocyclic ring with one or more members selected from the group consisting of the following (6-28-1) to (6-28-24) :   (6-28-1) lower alkyl groups,   (6-28-2) optionally substituted lower alkyl phenyl groups on the phenyl ring having one or more members selected from halogen atoms and optionally substituted lower alkoxy groups with one or more halogen atoms,   (6-28-3) lower alkyl naphthyl groups,     (6-28-4) phenyl lower alkyl lower alkylcarbamoyl groups,  (6-28-5) phenylcarbamoyl lower alkyl groups,  (6-28-6) phenyl lower alkoxycarbonyl groups,  (6-28-7) optionally substituted lower alkyl phenoxy groups on the phenyl ring with one or more members selected from the group consisting of halogen atoms and optionally substituted lower alkyl groups with one or more halogen atoms,  (6-28-8) biphenyl groups,   (6-28-9) optionally substituted phenyl groups on the phenyl ring having one or more halogen atoms,   (6-28-10) groups 2, 3-dihydroindenyl optionally substituted with one or more halogen atoms,   (6-28-11) benzothiazolyl groups optionally substituted by one or more halogen atoms,   (6-28-12) pyridyl groups optionally substituted by one or more halogen atoms,   (6-28-13) benzothienyl groups,  (6-28-14) benzoisothiazolyl groups,  (6-28-15) thienopyridyl groups,   (6-28-16) a carbamoyl group,   (6-28-17) phenyl lower alkoxy groups optionally substituted on the phenyl ring having one or more halogen atoms,   (6-28-18) phenoxy groups optionally substituted with one or more halogen atoms,   (6-28-19) optionally substituted benzoyl groups on the phenyl ring with one or more members selected from halogen atoms and lower alkoxy groups,   (6-28-20) optionally substituted anilino groups on the phenyl ring with one or more lower alkyl groups,  each lower alkyl substituent optionally being substituted with one or more halogen atoms,   (6-28-21) amino-substituted anilino groups having one or more lower alkyl groups,  and optionally also substituted on the phenyl ring with one or more halogen atoms,  (6-28-22) benzofuryl groups,  (6-28-23) naphthyl groups,   (6-28-24) an oxo group;  or R8 and R9 may be linked together to form,  together with the nitrogen atom to which they are attached,  an unsaturated 5 or 6 membered heterocyclic group,  the unsaturated heterocyclic group optionally being substituted on the heterocyclic ring with one or more members selected from the group consisting of the following (6-29-1) to (6-29-3):   (6-29-1) phenyl groups optionally substituted by one or more halogen atoms,   (6-29-2) groups 2, 3-dihydroindenyl,  (6-29-3) benzothienyl groups;  or instead,   R8 and R9 may be linked together to form,  together with the nitrogen atom to which they are attached,  a group 1, 2, 3, 4-tetrahydroquinolyl;  a group 1, 2, 3, 4-tetrahydroisoquinolyl,  a group 1, 3-dihydroisoindolyl;  an octahydropyrrole group [1, 2-a] pyrazinyl optionally substituted on the pyrazine ring with one or more lower alkyl groups;  or an 8-azabicyclo group [3, 2, 1] octyl optionally substituted on 8-azabicyclo [3, 2, 1] octyl with one or more phenoxy groups,  each phenoxy substituent being optionally substituted on the phenyl ring with one or more halogen atoms;   A2 is a lower alkylene group;   R10 is one of the following (7-1) to (7-44):   (7-1) a hydrogen atom,  (7-2) a lower alkyl group,   (7-3) an alkoxycarbonyl group optionally substituted by one or more halogen atoms,   (7-4) an optionally substituted benzoyl group on the phenyl ring with one or more members selected from the group consisting of lower alkyl groups optionally substituted with one or more halogen atoms;  a phenyl group;  halogen atoms;  a cyan group;  a phoxy group;  lower alkoxycarbonyl groups;  pyrazolyl groups;  and lower alkoxy groups optionally substituted with one or more halogen atoms,  (7-5) an alkanoyl group,   (7-6) a phenyl lower alkanoyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups,   (7-7) a lower cycloalkyl alkanoyl group,  (7-8) a phenyl group optionally substituted on the phenyl ring with one or more lower alkyl groups,   (7-9) a lower alkanoyl phenoxy group optionally substituted on the phenyl ring with one or more halogen atoms,   (7-10) a lower alkenylcarbonyl phenyl group,  (7-11) a pyridylcarbonyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups,  each lower alkyl substituent optionally being substituted with one or more halogen atoms,   (7-12) a furylcarbonyl group,   (7-13) a thienylcarbonyl group,   (7-14) a piperidinylcarbonyl group optionally substituted on the piperidine ring with one or more lower alkanoyl groups,   (7-15) a pyrrolidinylcarbonyl group optionally substituted on the pyrrolidine ring with one or more oxo groups,   (7-16) a tetrahydropyranylcarbonyl group,   (7-17) a naphthylcarbonyl group,  (7-18) an indolylcarbonyl group,  (7-19) a benzofurylcarbonyl group,   (7-20) a benzothienylcarbonyl group optionally substituted on the benzothiophene ring with one or more halogen atoms,  (7-21) a lower alkyl furyl group,   (7-22) a lower alkyl pyridyl group optionally substituted on the pyridine ring with one or more members selected from the group consisting of halogen atoms and lower alkyl groups,  each lower alkyl substituent optionally being substituted with one or more halogen atoms,   (7-23) a thienyl lower alkyl group optionally substituted on the thiophene ring with one or more halogen atoms,   (7-24) a lower alkyl phenyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of lower alkoxy groups optionally substituted with one or more halogen atoms;  a cyan group;  lower alkyl groups optionally substituted with one or more halogen atoms;  amino groups optionally substituted with one or more members selected from the group consisting of lower alkyl groups and lower alkanoyl groups;  halogen atoms;  lower alkoxycarbonyl groups;  lower alkanoyloxy groups;  lower alkylsulfonyl groups;  lower alkylthio groups;  and pyrrolidinyl groups,  (7-25) a lower alkyl thiazolyl group,   (7-26) a lower alkyl imidazole group optionally substituted on the imidazole ring with one or more lower alkyl groups,   (7-27) a pyrrolyl lower alkyl group optionally substituted on the pyrrol ring with one or more lower alkyl groups,  (7-28) a lower cycloalkyl alkyl group,  (7-29) a lower alkyl lower alkyl group,  (7-30) a phenoxycarbonyl group optionally substituted on the phenyl ring with one or more members selected from the group consisting of halogen atoms,  lower alkyl groups,  and lower alkoxy groups,   (7-31) a lower phenyl alkoxycarbonyl group optionally substituted on the phenyl ring with one or more halogen atoms,  (7-32) a naphthyloxycarbonyl group,  (7-33) a lower alkynyloxycarbonyl group,  (7-34) a cycloalkylcarbonyl group,  (7-35) a quinoxalinylcarbonyl group,  (7-36) a group -CO-NR13R14,     (7-37) a piperidinyl group optionally substituted on the piperidine ring with one or more lower alkyl groups,  (7-38) a cycloalkyl group,  (7-39) a tetrahydropyranyl group,   (7-40) a lower alkyl lower alkoxy group,   (7-41) a tetrahydro-2H-thiopyranyl group,  (7-42) a naphthyl group,  (7-43) a biphenyl group,   (7-44) a lower alkoxycarbonyl group lower alkylsilyl;   A3 is a lower alkylene group;   m is 0 or 1;   R 11 and R 12 each independently represent one of the following (8-1) to (8-5):   (8-1) a hydrogen atom,   (8-2) a lower alkyl group,   (8-3) a lower alkanoyl group,  (8-4) a lower phenyl alkanoyl group,   (8-5) a phenyl group optionally substituted on the phenyl ring with one or more halogen atoms;  or instead,   R11 and R12 may be linked together to form,  together with the nitrogen atom to which they are attached,  a 5- or 6-membered saturated heterocyclic group optionally containing one or more additional hetero atoms,  the heterocyclic group optionally being substituted with one to three members selected from the group consisting of the following (9-1) and (9-2):   (9-1) lower alkyl groups,  (9-2) a phenyl group;  and R 13 and R 14 each independently represent one of the following (10-1) to (10-3):   (10-1) a hydrogen atom,   (10-2) a lower alkyl group,  (10-3) a phenyl group,  or instead R13 and R14Can be linked together to form,  together with the nitrogen atom to which they are attached,  a 5- or 6-membered saturated heterocyclic group optionally containing one or more additional hetero atoms. Agent according to claim 1, characterized in that the disease associated with NF-κΒ- is selected from the group consisting of reperfusion disorders in ischemic diseases, exacerbation of organ transplantation prognosis or organ surgery, post-PTCA restenosis, cancer invasion and metastasis, and cachexia. Agent according to claim 1, characterized in that it is for regulating the transcription of cytokines and / or adhesion factors. Agent according to claim 3, characterized in that it is for inhibiting the activity of COX-2, TNF-α, and / or IL-8. Preventive or therapeutic agent for a disorder or disease associated with COX-2, characterized in that it comprises the carbostyril compound according to claim 1 or a salt thereof as an active ingredient. Strengthening of the anticancer effect, characterized in that it is for use in radiotherapy or chemotherapy comprising the carbostyril compound according to claim 1, or a salt thereof as an active ingredient. Radiosensitivity enhancer, characterized in that it is for use in radiotherapy comprising carbostyril compost according to claim 1, or a salt thereof as an active ingredient. A tumor-induced angiogenesis inhibitor, characterized in that it comprises the carbostyril compound according to claim 1, or a salt thereof as an active ingredient. Use of the carbostyril compound according to claim 1 or a salt thereof, characterized in that it is to produce a reinforcement in anticancer effect for use in radiotherapy or chemotherapy. Agent according to claim 1, characterized in that the carbostyril compound is represented by General Formula (1) wherein R 4 and R 5 each represent a hydrogen atom. Agent according to claim 11, characterized in that the carbostyril compound is represented by General Formula (1) wherein a group of Formula <RTIgt; and X are as defined according to claim 1 above, is attached to the 3, 4, 5, 6, 7 or 8 position of the carbostyril backbone. Agent according to Claim 12, characterized in that the carbostyril compound is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a single bond, and the group of Formula, wherein R 3, A and X are as defined according to claim 1 above, is attached to position 5 or 6 of the carbostyril backbone. Agent according to Claim 11 or 12, characterized in that the carbostyril compound is represented by General Formula (1) wherein A is a lower alkylene group or a lower alkydylene group. Agent according to claim 13, characterized in that the carbostyril compound is represented by the general formula (1) wherein R1 is one of (1-2), (1-3), (1-4) , (1-6), (1-10), (1-12), (1-13), (1-18) and (1-21) as defined according to claim 1 above. Agent according to claim 14, characterized in that the carbostyril compound is represented by General Formula (1) wherein the group of Formula <RTIgt; and X are as defined according to claim 1 above, is attached to position 5 of the carbostyril backbone. Agent according to claim 15, characterized in that the carbostyril compound is represented by General Formula (1) wherein A is a lower alkylene group, R1 is a lower alkyl group, R2 is a hydrogen atom or a lower alkoxy group, R3 is a hydrogen atom, and X is an oxygen atom or a sulfur atom. Agent according to claim 1, characterized in that the carbostyril compound is represented by General Formula (1) wherein A is a lower alkylene group. An agent according to claim 17, characterized in that the carbostyril compound is represented by General Formula (1) wherein the bond between positions 3 and 4 of the carbostyril backbone is a single bond or a double bond, and R4 and R5 each represent a hydrogen atom. Agent according to claim 1, characterized in that the carbostyril compound is selected from the group consisting of the following compounds: [5- [1- (biphenyl-4-ylmethyl) -8-methoxy-2-oxo]. 1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione, [5- [1- (4-chlorobenzyl) -8-methoxy-2-oxo-1,2,3, 4-Tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione, [5- [1- (4-bromobenzyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-one ylmethyl] thiazolidine-2,4-dione, [5- [1- (2-naphthylmethyl) -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine 2,4-dione, 5- {1- [4- (heptyloxycarbonylamino) benzyl] -8-methoxy-2-oxo-1,2,3,4-tetrahydroquinoline-5-ylmethyl} thiazolidine-2,4-one dione, [5- [1- (1-biphenyl-4-ylpiperidin-4-ylmethyl) -2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl] thiazolidine-2,4-dione, [5 - {1- [1- (4-methylphenyl) piperidin-4-ylmethyl] -2-oxo-1,2,3,4-tetrahydroquinolin-5-ylmethyl} thiazolidine-2,4-dione, [5- {1- [4- (2-chlorobenzyloxycarbonylamino) benzyl] -8-methoxy-2-oxo-1,2,3,4-tetraethyl - droquinolin-5-ylmethyl} thiazolidin-2,4-dione, [1- (biphenyl-4-ylmethyl) -8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-one dihydro-quinolin-2-one, [8-methoxy-1-methyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one, [8- methoxy-1- (3-methylbutyl) -5- (4-oxo-24oxythiazolidin-5-ylmethyl) -3,4-dihydro-phenylolin-2-one, [1-propyl-8-methoxy-5- (4 -oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolinone, [1-isobutyl-8-methoxy-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3, 4-dihydro-1H-qui [2-one, [8-methoxy-14-ethyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinonone, and [1- (4-phenylthiomethyl) benzyl-5- (4-oxo-2-thioxothiazolidin-5-ylmethyl) -3,4-dihydro-1H-quinolin-2-one; or a salt of these.